{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,14]],"date-time":"2026-10-14T22:35:46Z","timestamp":1792017346163,"version":"4.4.0"},"reference-count":150,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2025,4,1]],"date-time":"2025-04-01T00:00:00Z","timestamp":1743465600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/100016045","name":"University of Central Punjab","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100016045","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001427","name":"All India Council for Technical Education","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100001427","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic Chemistry"],"published-print":{"date-parts":[[2025,4]]},"DOI":"10.1016\/j.bioorg.2025.108273","type":"journal-article","created":{"date-parts":[[2025,2,17]],"date-time":"2025-02-17T11:08:13Z","timestamp":1739790493000},"page":"108273","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":11,"special_numbering":"C","title":["Recent developments of pyrimidine appended HIV-1 non-nucleoside reverse transcriptase inhibitors"],"prefix":"10.1016","volume":"157","author":[{"given":"S. Maheen Abdul","family":"Rahman","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gurpreet","family":"Singh","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mhd Shabbu","family":"Khan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Arun Kumar","family":"Balasubramaniam","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vikramdeep","family":"Monga","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.bioorg.2025.108273_bb0005","doi-asserted-by":"crossref","first-page":"2529","DOI":"10.1002\/rmv.2529","article-title":"Pharmacological advances in anti-retroviral therapy for human immunodeficiency virus-1 infection: a comprehensive review","volume":"34","author":"Azzman","year":"2024","journal-title":"Rev. Med. Virol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0010","author":"Hiv.Gov, Global HIV Data and Statistics"},{"key":"10.1016\/j.bioorg.2025.108273_bb0015","series-title":"Highly Active Antiretroviral Therapy (HAART) [Updated 2023 Jul 3]. In: StatPearls [Internet]. Treasure Island (FL)","author":"Eggleton","year":"2024"},{"key":"10.1016\/j.bioorg.2025.108273_bb0020","doi-asserted-by":"crossref","first-page":"400","DOI":"10.1080\/21505594.2020.1760443","article-title":"Mechanisms underlying antiretroviral drugs in different cellular reservoirs with a focus on macrophages","volume":"11","author":"Aquaro","year":"2020","journal-title":"Virulence"},{"key":"10.1016\/j.bioorg.2025.108273_bb0025","article-title":"Challenges of HIV management in an aging population","volume":"22","author":"Thomas","year":"2024","journal-title":"Curr. HIV\/AIDS Rep."},{"key":"10.1016\/j.bioorg.2025.108273_bb0030","doi-asserted-by":"crossref","first-page":"25","DOI":"10.1016\/j.antiviral.2009.10.007","article-title":"Current status and challenges of antiretroviral research and therapy","volume":"85","author":"Est\u00e9","year":"2010","journal-title":"Antivir. Res."},{"key":"10.1016\/j.bioorg.2025.108273_bb0035","doi-asserted-by":"crossref","first-page":"1111","DOI":"10.1592\/phco.26.8.1111","article-title":"An update and review of antiretroviral therapy","volume":"26","author":"Piacenti","year":"2006","journal-title":"Pharmacotherapy"},{"key":"10.1016\/j.bioorg.2025.108273_bb0040","first-page":"2789","article-title":"Combination antiretroviral therapy for HIV infection","volume":"57","author":"Maenza","year":"1998","journal-title":"Am. Fam. Physician"},{"key":"10.1016\/j.bioorg.2025.108273_bb0045","doi-asserted-by":"crossref","first-page":"32","DOI":"10.1097\/COH.0000000000000712","article-title":"Fostemsavir: a first-in-class HIV-1 attachment inhibitor","volume":"17","author":"Grant","year":"2022","journal-title":"Curr. Opin. HIV AIDS"},{"key":"10.1016\/j.bioorg.2025.108273_bb0050","doi-asserted-by":"crossref","first-page":"135","DOI":"10.1517\/14728214.2012.673584","article-title":"CCR5 inhibitors: emergence, success, and challenges","volume":"17","author":"Maeda","year":"2012","journal-title":"Expert Opin. Emerg. Drugs"},{"key":"10.1016\/j.bioorg.2025.108273_bb0055","doi-asserted-by":"crossref","first-page":"2175","DOI":"10.1056\/NEJMoa035026","article-title":"Study group Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in north and South America","volume":"348","author":"Lalezari","year":"2003","journal-title":"N. Engl. J. Med."},{"key":"10.1016\/j.bioorg.2025.108273_bb0060","doi-asserted-by":"crossref","first-page":"403","DOI":"10.1080\/14656566.2020.1843635","article-title":"An evaluation of cabotegravir for HIV treatment and prevention","volume":"22","author":"Canetti","year":"2021","journal-title":"Expert. Opin. Pharmacother."},{"key":"10.1016\/j.bioorg.2025.108273_bb0065","doi-asserted-by":"crossref","first-page":"981","DOI":"10.1007\/s40262-013-0093-2","article-title":"Clinical pharmacokinetic, pharmacodynamic, and drug-interaction profile of the integrase inhibitor dolutegravir","volume":"52","author":"Cottrell","year":"2013","journal-title":"Clin. Pharmacokinet."},{"key":"10.1016\/j.bioorg.2025.108273_bb0070","doi-asserted-by":"crossref","first-page":"1209","DOI":"10.3390\/v1031209","article-title":"Current and novel inhibitors of HIV protease","volume":"1","author":"Pokorn\u00e1","year":"2009","journal-title":"Viruses"},{"key":"10.1016\/j.bioorg.2025.108273_bb0075","doi-asserted-by":"crossref","first-page":"205","DOI":"10.3390\/v13020205","article-title":"Integrase Strand transfer inhibitors are effective anti-HIV drugs","volume":"13","author":"Smith","year":"2021","journal-title":"Viruses"},{"key":"10.1016\/j.bioorg.2025.108273_bb0080","doi-asserted-by":"crossref","first-page":"395","DOI":"10.1517\/13543784.2012.658914","article-title":"Elvitegravir: a once-daily inhibitor of HIV-1 integrase","volume":"21","author":"Wills","year":"2012","journal-title":"Expert Opin. Investig. Drugs"},{"key":"10.1016\/j.bioorg.2025.108273_bb0085","doi-asserted-by":"crossref","first-page":"2581","DOI":"10.2147\/OTT.S136484","article-title":"The HIV protease inhibitor, nelfinavir, as a novel therapeutic approach for the treatment of refractory pediatric leukemia","volume":"10","author":"Meier-Stephenson","year":"2017","journal-title":"Onco. Targets Ther."},{"key":"10.1016\/j.bioorg.2025.108273_bb0090","doi-asserted-by":"crossref","first-page":"189","DOI":"10.1007\/s40265-020-01258-3","article-title":"Ibalizumab: a review in multidrug-resistant HIV-1 infection","volume":"80","author":"Blair","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.bioorg.2025.108273_bb0095","series-title":"Antiviral Nucleoside Reverse Transcriptase Inhibitor","author":"Wang","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0100","series-title":"Thiazolo-Pyrimidine HIV-1 Reverse Transcriptase Inhibitor, a Preparation Method Therefor, and Uses Thereof, Shan Dong Univ., U.S. Patent No. 11225491B2","author":"Liu","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0105","series-title":"Compounds Useful in HIV Therapy, Glaxosmithkline IP Dev. Ltd., U.S. Patent No. 11274102B2","author":"Favre","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0110","series-title":"Combinations Comprising 5-Phenoxy-3H-Pyrimidin-4-One Derivatives and their Use for the Prophylaxis or Treatment of Infection by HIV","author":"Kenneth","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0115","series-title":"Biphenyl-Containing Diarylpyrimido Compounds, Pharmaceutically-Acceptable Salts Thereof, Composition And Preparation Thereof, University of Fudan, U.S. Patent No.11447501B2","author":"Chen","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0120","series-title":"Substituted 1,2,3,3a,4,5,7,9,13,13a-Decahydropyrido[1\u2032,2\u2032:4,5]Pyrazino[1,2-a]Pyrrolo[1,2-c]Pyrimidines Having HIV Integrase Inhibitory Activity","author":"J. Brian","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0125","series-title":"Barrett, Sunose, Kamaldeep, 4-[[(7-Aminopyrazolo[1,5-A]Pyrimidin-5-Yl)Amino]Methyl]Piperidin-3-ol Compounds as CDK Inhibitors, Carrick Therapeutics Ltd, Cancer Research Tech Ltd, IP2IPO Innovations Ltd., EP. Patent No. EP3684769B1","author":"Bahl","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0130","series-title":"Humanized Anti-Human PD-1 Antibody, US, OSE immunotherapies, U.S. Patent No. 20210355225A1","author":"Poirier","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0135","series-title":"Hydrogel Prodrug for Treatment","author":"Fisher","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0140","series-title":"Use of TREM-1 Inhibitors for Treatment, Elimination and Eradication of HIV-1 Infection","author":"Schinazi Raymond","year":"2021"},{"key":"10.1016\/j.bioorg.2025.108273_bb0145","series-title":"Antiviral JAK inhibitors useful in treating or preventing coronaviridae infections, Univ. Emory, U.S. Patent 11045474","author":"Gavegnano","year":"2021"},{"key":"10.1016\/j.bioorg.2025.108273_bb0150","series-title":"Jianmin, 4\u2019-Substituted nucleoside-derivatives as HIV reverse transcriptase inhibitors, Merck Sharp & Dohme, EP. Patent No. 3122752B1","author":"Girijavallabhan Vinay","year":"2021"},{"key":"10.1016\/j.bioorg.2025.108273_bb0155","series-title":"Fatty Acid Synthase Inhibitors, Univ Duke","author":"Kwiek","year":"2021"},{"key":"10.1016\/j.bioorg.2025.108273_bb0160","series-title":"Pyrazolopyridinamines as MKNK1 and MKNK02 Inhibitors,Bayer Pharma AG, EP. Patent No. 3233866B1","author":"Giese","year":"2021"},{"key":"10.1016\/j.bioorg.2025.108273_bb0165","series-title":"Biphenyl-Containing Diarylpyrimido Compounds, Pharmaceutically-Acceptable Salts Thereof, Composition and Preparation Thereof","author":"Chen","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0170","series-title":"Solid Forms of a Kynurenine-3-Monooxygenase Inhibitor, Chdi Foundation Inc., U.S. Patent No. 11173156B2","author":"Toledo-Sherman Leticia","year":"2021"},{"key":"10.1016\/j.bioorg.2025.108273_bb0175","series-title":"Salt of 4[[4-[[4-(2-Cyanoethenyl)-2,6-dimethylphenyl]Amino]-2-Pyrimidinyl]amino] benzonitrile, Janssen Pharmaceutica Nv. EP. Patent No. 1632232B3","author":"Stevens","year":"2022"},{"key":"10.1016\/j.bioorg.2025.108273_bb0180","doi-asserted-by":"crossref","first-page":"2102","DOI":"10.1021\/acs.jmedchem.2c01875","article-title":"Structure-based optimization of 2,4,5-trisubstituted pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors: exploiting the tolerant regions of the non-nucleoside reverse transcriptase inhibitors\u2019 binding pocket","volume":"66","author":"Zhao","year":"2023","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0185","doi-asserted-by":"crossref","first-page":"371","DOI":"10.1038\/nrmicro1389","article-title":"Parallels among positive-strand RNA viruses, reverse-transcribing viruses, and double-stranded RNA viruses","volume":"4","author":"Ahlquist","year":"2006","journal-title":"Nat. Rev. Microbiol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0190","series-title":"Structure and organization of virus genomes","first-page":"1","author":"Chaitanya","year":"2019"},{"key":"10.1016\/j.bioorg.2025.108273_bb0195","doi-asserted-by":"crossref","first-page":"275","DOI":"10.1146\/annurev.cb.08.110192.001423","article-title":"Retroviral reverse transcription and integration: progress and problems","volume":"8","author":"Whitcomb","year":"1992","journal-title":"Annu. Rev. Cell Biol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0200","doi-asserted-by":"crossref","first-page":"39","DOI":"10.1016\/j.antiviral.2009.09.014","article-title":"Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine","volume":"85","author":"Cihlar","year":"2010","journal-title":"Antivir. Res."},{"key":"10.1016\/j.bioorg.2025.108273_bb0205","first-page":"411","article-title":"Nucleotide reverse transcriptase inhibitors: a thorough review, present status and future perspective as HIV therapeutics","volume":"15","author":"Holec","year":"2017","journal-title":"Curr. HIV Res."},{"key":"10.1016\/j.bioorg.2025.108273_bb0210","doi-asserted-by":"crossref","first-page":"40850","DOI":"10.1074\/jbc.R112.389056","article-title":"Human immunodeficiency virus reverse transcriptase: 25 years of research, drug discovery, and promise","volume":"287","author":"Le Grice","year":"2012","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0215","doi-asserted-by":"crossref","first-page":"4535","DOI":"10.1093\/emboj\/17.15.4535","article-title":"The structure of HIV-1 reverse transcriptase complexed with an RNA pseudoknot inhibitor","volume":"17","author":"Jaeger","year":"1998","journal-title":"EMBO J."},{"key":"10.1016\/j.bioorg.2025.108273_bb0220","doi-asserted-by":"crossref","first-page":"136","DOI":"10.1016\/j.tim.2012.11.006","article-title":"HIV gag polyprotein: processing and early viral particle assembly","volume":"21","author":"Bell","year":"2013","journal-title":"Trends Microbiol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0225","doi-asserted-by":"crossref","first-page":"88","DOI":"10.1126\/science.1707186","article-title":"Crystal structure of the ribonuclease H domain of HIV-1 reverse transcriptase","volume":"252","author":"Davies","year":"1991","journal-title":"Science"},{"key":"10.1016\/j.bioorg.2025.108273_bb0230","doi-asserted-by":"crossref","first-page":"693","DOI":"10.1016\/j.jmb.2008.10.071","article-title":"Structure and function of HIV-1 reverse transcriptase: molecular mechanisms of polymerization and inhibition","volume":"385","author":"Sarafianos","year":"2009","journal-title":"J. Mol. Biol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0235","doi-asserted-by":"crossref","first-page":"4851","DOI":"10.1021\/acs.jmedchem.8b00843","article-title":"The journey of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) from lab to clinic","volume":"62","author":"Namasivayam","year":"2019","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0240","doi-asserted-by":"crossref","first-page":"14372","DOI":"10.1111\/cbdd.14372","article-title":"Current insights and molecular docking studies of HIV-1 reverse transcriptase inhibitors","volume":"103","author":"Singh","year":"2024","journal-title":"Chem. Biol. Drug Des."},{"key":"10.1016\/j.bioorg.2025.108273_bb0245","doi-asserted-by":"crossref","first-page":"1761","DOI":"10.1021\/acs.jmedchem.2c01574","article-title":"Design and synthesis of novel HIV-1 NNRTIs with bicyclic cores and with improved physicochemical properties","volume":"66","author":"Prener","year":"2023","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0250","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2022.114554","article-title":"HIV nucleoside reverse transcriptase inhibitors","volume":"240","author":"Amblard","year":"2022","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0255","doi-asserted-by":"crossref","first-page":"1411","DOI":"10.1126\/science.1701568","article-title":"Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor","volume":"250","author":"Merluzzi","year":"1990","journal-title":"Science"},{"key":"10.1016\/j.bioorg.2025.108273_bb0260","doi-asserted-by":"crossref","first-page":"75","DOI":"10.1016\/j.antiviral.2009.09.008","article-title":"Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: a review of the last 20 years (1989-2009)","volume":"85","author":"de B\u00e9thune","year":"2010","journal-title":"Antivir. Res."},{"key":"10.1016\/j.bioorg.2025.108273_bb0265","doi-asserted-by":"crossref","first-page":"723","DOI":"10.1007\/s00253-007-0919-7","article-title":"HIV-1 reverse transcriptase inhibitors","volume":"75","author":"El Safadi","year":"2007","journal-title":"Appl. Microbiol. Biotechnol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0270","doi-asserted-by":"crossref","first-page":"323","DOI":"10.2174\/1570162043351093","article-title":"Conformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding","volume":"2","author":"Sluis-Cremer","year":"2004","journal-title":"Curr. HIV Res."},{"key":"10.1016\/j.bioorg.2025.108273_bb0275","doi-asserted-by":"crossref","first-page":"123","DOI":"10.1038\/373123a0","article-title":"Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection","volume":"373","author":"Ho","year":"1995","journal-title":"Nature"},{"key":"10.1016\/j.bioorg.2025.108273_bb0280","doi-asserted-by":"crossref","first-page":"117","DOI":"10.1038\/373117a0","article-title":"Viral dynamics in human immunodeficiency virus type 1 infection","volume":"373","author":"Wei","year":"1995","journal-title":"Nature"},{"key":"10.1016\/j.bioorg.2025.108273_bb0285","doi-asserted-by":"crossref","first-page":"5000","DOI":"10.1128\/AAC.00591-12","article-title":"Antiviral drug resistance and the need for development of new HIV-1 reverse transcriptase inhibitors","volume":"56","author":"Asahchop","year":"2012","journal-title":"Antimicrob. Agents Chemother."},{"key":"10.1016\/j.bioorg.2025.108273_bb0290","doi-asserted-by":"crossref","first-page":"1075","DOI":"10.1021\/acsmedchemlett.5b00254","article-title":"Potent inhibitors active against HIV reverse transcriptase with K101P, a mutation conferring rilpivirine resistance","volume":"6","author":"Gray","year":"2015","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0295","first-page":"915","article-title":"The phenomenon of antiretroviral drug resistance in the context of human immunodeficiency virus treatment: dynamic and ever evolving subject matter","volume":"12","author":"Apetroaei","year":"2024","journal-title":"Biomed"},{"key":"10.1016\/j.bioorg.2025.108273_bb0300","doi-asserted-by":"crossref","first-page":"7589","DOI":"10.1128\/JVI.00302-14","article-title":"Mutations in HIV-1 reverse transcriptase affect the errors made in a single cycle of viral replication","volume":"88","author":"Abram","year":"2014","journal-title":"J. Virol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0305","series-title":"Canadian Zidovudine Multi-Centre Study Group. AIDS","first-page":"411","article-title":"Isolation of drug-resistant variants of HIV-1 from patients on long-term zidovudine therapy","volume":"vol. 3","author":"Rooke","year":"1989"},{"key":"10.1016\/j.bioorg.2025.108273_bb0310","doi-asserted-by":"crossref","first-page":"705","DOI":"10.1097\/00002030-199807000-00006","article-title":"The M184V mutation in HIV-1 reverse transcriptase (RT) conferring lamivudine resistance does not result in broad cross-resistance to nucleoside analogue RT inhibitors","volume":"12","author":"Miller","year":"1998","journal-title":"AIDS (London, England)"},{"key":"10.1016\/j.bioorg.2025.108273_bb0315","first-page":"83","article-title":"Abacavir\/lamivudine combination in the treatment of HIV: a review","volume":"6","author":"Sivasubramanian","year":"2010","journal-title":"Ther. Clin. Risk Manag."},{"key":"10.1016\/j.bioorg.2025.108273_bb0320","doi-asserted-by":"crossref","first-page":"13965","DOI":"10.1074\/jbc.M009837200","article-title":"The valine-to-threonine 75 substitution in human immunodeficiency virus type 1 reverse transcriptase and its relation with stavudine resistance","volume":"276","author":"Selmi","year":"2001","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0325","doi-asserted-by":"crossref","first-page":"157","DOI":"10.1128\/AAC.00904-07","article-title":"Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 reverse transcriptase facilitates dual resistance to zidovudine and lamivudine","volume":"52","author":"Zelina","year":"2008","journal-title":"Antimicrob. Agents Chemother."},{"key":"10.1016\/j.bioorg.2025.108273_bb0330","doi-asserted-by":"crossref","first-page":"F9","DOI":"10.1097\/01.aids.0000232228.88511.0b","article-title":"HIV-1 subtype C viruses rapidly develop K65R resistance to tenofovir in cell culture","volume":"20","author":"Brenner","year":"2006","journal-title":"AIDS (London, England)"},{"key":"10.1016\/j.bioorg.2025.108273_bb0335","doi-asserted-by":"crossref","first-page":"813","DOI":"10.1080\/17425255.2019.1673367","article-title":"Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment","volume":"15","author":"Wang","year":"2019","journal-title":"Expert Opin. Drug Metab. Toxicol."},{"issue":"1","key":"10.1016\/j.bioorg.2025.108273_bb0340","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0147225","article-title":"Ribonuclease H\/DNA polymerase HIV-1 reverse transcriptase dual inhibitor: mechanistic studies on the allosteric mode of action of isatin-based compound RMNC6","volume":"11","author":"Corona","year":"2016","journal-title":"PLoS One"},{"key":"10.1016\/j.bioorg.2025.108273_bb0345","doi-asserted-by":"crossref","first-page":"6611","DOI":"10.1039\/C6OB00936K","article-title":"Modern advances in heterocyclic chemistry in drug discovery","volume":"14","author":"Taylor","year":"2016","journal-title":"Org. Biomol. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0350","doi-asserted-by":"crossref","first-page":"1047","DOI":"10.1016\/j.jtusci.2017.05.005","article-title":"Proficient synthesis of bioactive annulated pyrimidine derivatives: a review","volume":"11","author":"Bhat","year":"2017","journal-title":"J. Taibah Univ. Sci."},{"key":"10.1016\/j.bioorg.2025.108273_bb0355","doi-asserted-by":"crossref","first-page":"7166","DOI":"10.2174\/0929867325666180904125400","article-title":"Pyridine and pyrimidine derivatives as privileged scaffolds in biologically active agents","volume":"26","author":"Chiacchio","year":"2019","journal-title":"Curr. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0360","doi-asserted-by":"crossref","first-page":"1112","DOI":"10.1039\/D0MD00227E","article-title":"Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold","volume":"11","author":"Baillache","year":"2020","journal-title":"RSC Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0365","doi-asserted-by":"crossref","first-page":"5657","DOI":"10.1016\/j.bmc.2013.07.027","article-title":"Medicinal attributes of pyrazolo[3,4-d]pyrimidines: a review","volume":"21","author":"Chauhan","year":"2013","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0370","doi-asserted-by":"crossref","first-page":"926","DOI":"10.2174\/1871527321666220107154617","article-title":"Structural activity relationship based medicinal perspectives of pyrimidine derivatives as anti-Alzheimer\u2019s agents: a comprehensive review","volume":"21","author":"Das","year":"2022","journal-title":"CNS Neurol. Disord. Drug Targets"},{"key":"10.1016\/j.bioorg.2025.108273_bb0375","doi-asserted-by":"crossref","DOI":"10.1016\/j.arabjc.2022.104378","article-title":"Current scenario on non-nucleoside reverse transcriptase inhibitors (2018-present)","volume":"15","author":"Deng","year":"2022","journal-title":"Arab. J. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0380","doi-asserted-by":"crossref","first-page":"202100744","DOI":"10.1002\/ajoc.202100744","article-title":"An overview on indole aryl sulfide\/sulfone (IAS) as anti-HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)","volume":"11","author":"Sinha","year":"2022","journal-title":"Asian J. Org. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0385","doi-asserted-by":"crossref","first-page":"961","DOI":"10.1016\/j.apsb.2019.11.010","article-title":"Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years","volume":"10","author":"Zhuang","year":"2020","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.bioorg.2025.108273_bb0390","doi-asserted-by":"crossref","first-page":"248","DOI":"10.1016\/j.ejmech.2017.02.054","article-title":"Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase","volume":"130","author":"Sonar","year":"2017","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0395","doi-asserted-by":"crossref","first-page":"2430","DOI":"10.1080\/07391102.2020.1748111","article-title":"Anti-HIV potential of diarylpyrimidine derivatives as non-nucleoside reverse transcriptase inhibitors: design, synthesis, docking, TOPKAT analysis and molecular dynamics simulations","volume":"39","author":"Singh","year":"2021","journal-title":"J. Biomol. Struct. Dyn."},{"key":"10.1016\/j.bioorg.2025.108273_bb0400","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.113051","article-title":"Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties","volume":"213","author":"Jiang","year":"2021","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0405","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.112549","article-title":"Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors","volume":"202","author":"Chen","year":"2020","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0410","doi-asserted-by":"crossref","first-page":"1581","DOI":"10.3390\/molecules25071581","article-title":"Scaffold hopping in discovery of HIV-1 non-nucleoside reverse transcriptase inhibitors: from CH(CN)-DABOs to CH(CN)-DAPYs","volume":"25","author":"Li","year":"2020","journal-title":"Molecules"},{"key":"10.1016\/j.bioorg.2025.108273_bb0415","doi-asserted-by":"crossref","first-page":"2083","DOI":"10.1021\/acs.jmedchem.8b01729","volume":"62","author":"Huang","year":"2019","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0420","doi-asserted-by":"crossref","DOI":"10.1177\/2040206619826265","article-title":"Synthesis and anti-human immunodeficiency virus activity of substituted (o,o-difluorophenyl)-linked-pyrimidines as potent non-nucleoside reverse transcriptase inhibitors","volume":"27","author":"\u010cechov\u00e1","year":"2019","journal-title":"Antivir. Chem. Chemother."},{"key":"10.1016\/j.bioorg.2025.108273_bb0425","doi-asserted-by":"crossref","first-page":"726","DOI":"10.1016\/j.ejmech.2018.01.016","article-title":"Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1","volume":"145","author":"Jin","year":"2018","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0430","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmc.2021.116195","article-title":"Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs","volume":"40","author":"Gao","year":"2021","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0435","doi-asserted-by":"crossref","DOI":"10.1016\/j.bioorg.2020.103595","article-title":"Pharmacophore-fusing design of pyrimidine sulfonylacetanilides as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase","volume":"96","author":"Sang","year":"2020","journal-title":"Bioorg. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0440","doi-asserted-by":"crossref","DOI":"10.1016\/j.bioorg.2022.105880","article-title":"Structure-based design of [(2-Hydroxyethoxy)methyl]-6-(phenylthio)-thymine derivatives as nonnucleoside HIV-1 reverse transcriptase inhibitors: from HEPTs to Sulfinyl-substituted HEPTs","volume":"126","author":"Hao","year":"2022","journal-title":"Bioorg. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0445","doi-asserted-by":"crossref","first-page":"4239","DOI":"10.1021\/acs.jmedchem.1c00268","article-title":"2,4,5-trisubstituted pyrimidines as potent HIV-1 NNRTIs: rational design, synthesis, activity evaluation, and crystallographic Studie","volume":"64","author":"Kang","year":"2021","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0450","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2021.113868","article-title":"Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel","volume":"226","author":"Jin","year":"2021","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0455","doi-asserted-by":"crossref","DOI":"10.1016\/j.bioorg.2021.104905","article-title":"Chemical space exploration of novel naphthyl-carboxamide-diarylpyrimidine derivatives with potent anti-HIV-1 activity","volume":"111","author":"Sang","year":"2021","journal-title":"Bioorg. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0460","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2022.114957","article-title":"Disubstituted pyrimidine-5-carboxamide derivatives as novel HIV-1 NNRTIs: crystallographic overlay-based molecular design, synthesis, and biological evaluation","volume":"246","author":"Feng","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0465","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.113063","article-title":"Design, synthesis, and evaluation of \u201cdual-site\u201d-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase","volume":"211","author":"Feng","year":"2021","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0470","first-page":"152","article-title":"Synthesis of novel pyridine and pyrimidine derivatives as potential inhibitors of HIV-1 reverse transcriptase using palladium-catalysed C-N cross-coupling and nucleophilic aromatic substitution reactions","author":"Changunda","year":"2020","journal-title":"J. Organomet. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0475","doi-asserted-by":"crossref","first-page":"1020","DOI":"10.1016\/j.cclet.2020.09.035","article-title":"Structure-based linker optimization of 6-(2-cyclohexyl-1-alkyl)-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors","volume":"32","author":"Li","year":"2021","journal-title":"Chin. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0480","doi-asserted-by":"crossref","first-page":"63","DOI":"10.1021\/ml1002162","article-title":"N-3 hydroxylation of pyrimidine-2,4-diones yields dual inhibitors of HIV reverse transcriptase and integrase","volume":"2","author":"Tang","year":"2011","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0485","doi-asserted-by":"crossref","first-page":"168","DOI":"10.1016\/j.ejmech.2017.01.041","article-title":"6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverase transcriptase: impacts of the 3-OH on inhibiting RNase H and polymerase","volume":"128","author":"Tang","year":"2017","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0490","article-title":"Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1","volume":"99","author":"Yang","year":"2020","journal-title":"Bioorg. Cehem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0495","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2019.111864","article-title":"Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: design, synthesis and biological activities","volume":"186","author":"Xiao","year":"2020","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0500","doi-asserted-by":"crossref","first-page":"1718","DOI":"10.3390\/molecules24091718","article-title":"Pyrimidine 2,4-Diones in the Design of new HIV RT inhibitors","volume":"24","author":"Romeo","year":"2019","journal-title":"Molecules"},{"key":"10.1016\/j.bioorg.2025.108273_bb0505","doi-asserted-by":"crossref","first-page":"680","DOI":"10.1016\/j.ejmech.2018.07.035","article-title":"6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H","volume":"156","author":"Wang","year":"2018","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0510","doi-asserted-by":"crossref","first-page":"652","DOI":"10.1016\/j.ejmech.2018.07.039","article-title":"6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity","volume":"156","author":"Wang","year":"2018","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0515","doi-asserted-by":"crossref","first-page":"2648","DOI":"10.1021\/acs.jmedchem.5b01879","article-title":"3-Hydroxypyrimidine-2,4-diones as selective active site inhibitors of HIV reverse transcriptase-associated RNase H: design, synthesis, and biochemical evaluation","volume":"59","author":"Tang","year":"2016","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0520","doi-asserted-by":"crossref","first-page":"5045","DOI":"10.1021\/acs.jmedchem.7b00440","article-title":"Double-winged 3-hydroxypyrimidine-2,4-diones: potent and selective inhibition against HIV-1 RNase H with significant antiviral activity","volume":"60","author":"Vernekar","year":"2017","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0525","doi-asserted-by":"crossref","first-page":"2051","DOI":"10.1016\/j.bmc.2018.03.003","article-title":"The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2","volume":"26","author":"Lu","year":"2018","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0530","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmc.2021.116239","article-title":"Exploiting the hydrophobic channel of the NNIBP: discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses","volume":"42","author":"Fu","year":"2021","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0535","doi-asserted-by":"crossref","first-page":"3491","DOI":"10.1016\/j.bmcl.2018.10.010","article-title":"Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine","volume":"28","author":"Jin","year":"2018","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0540","doi-asserted-by":"crossref","first-page":"5067","DOI":"10.1021\/acs.jmedchem.1c00128","article-title":"Hydrophobic pocket occupation design of difluoro-biphenyl-diarylpyrimidines as non-nucleoside HIV-1 reverse transcriptase inhibitors: from N-alkylation to methyl hopping on the pyrimidine ring","volume":"64","author":"Ding","year":"2021","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0545","doi-asserted-by":"crossref","first-page":"1192","DOI":"10.1016\/j.apsb.2022.08.017","article-title":"Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: boosting the safety and metabolic stability","volume":"13","author":"Jin","year":"2023","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.bioorg.2025.108273_bb0550","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2023.115114","article-title":"Hybrids of delavirdine and piperdin-4-yl-aminopyrimidines (DPAPYs) as potent HIV-1 NNRTIs: design, synthesis and biological activities","volume":"248","author":"Ming","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0555","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2023.115605","article-title":"Discovery of novel diarypyrimidine derivatives bearing six-membered non-aromatic heterocycles as potent HIV-1 NNRTIs with improved anti-resistance and drug-like profiles","volume":"258","author":"Jiang","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0560","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2022.115045","article-title":"Identification of \"dual-site\"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase","volume":"247","author":"Feng","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0565","doi-asserted-by":"crossref","first-page":"83","DOI":"10.1038\/s42004-023-00888-4","article-title":"Discovery of diarylpyrimidine derivatives bearing piperazine sulfonyl as potent HIV-1 nonnucleoside reverse transcriptase inhibitors","volume":"6","author":"Jiang","year":"2023","journal-title":"Commun. Chem."},{"issue":"2024","key":"10.1016\/j.bioorg.2025.108273_bb0570","article-title":"Discovery of 2,4,6-trisubstituted pyrimidine derivatives as novel potent HIV-1 NNRTIs by exploiting the tolerant region II of the NNIBP","volume":"277","author":"Zhou","year":"2024","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0575","article-title":"Structure-based discovery of novel piperidine-biphenyl-DAPY derivatives as non-nucleoside reverse transcriptase inhibitors featuring improved potency, safety, and selectivity: from piperazine-biphenyl-DAPYs to piperidine-biphenyl-DAPYs","author":"Huang","year":"2024","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0580","doi-asserted-by":"crossref","first-page":"29502","DOI":"10.1002\/jmv.29502","article-title":"Structure-based design of diarylpyrimidines and triarylpyrimidines as potent HIV-1 NNRTIs with improved metabolic stability and drug resistance profiles","volume":"96","author":"Xie","year":"2024","journal-title":"J. Med. Virol."},{"key":"10.1016\/j.bioorg.2025.108273_bb0585","doi-asserted-by":"crossref","first-page":"754","DOI":"10.1016\/j.ejmech.2015.01.042","article-title":"Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches","volume":"92","author":"Huang","year":"2015","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0590","doi-asserted-by":"crossref","first-page":"67","DOI":"10.1111\/cbdd.13760","article-title":"Design, synthesis, and biological evaluation of piperidinyl-substituted [1,2,4]triazolo[1,5-a]pyrimidine derivatives as potential anti-HIV-1 agents with reduced cytotoxicity","volume":"97","author":"Huang","year":"2021","journal-title":"Chem. Biol. Drug Des."},{"key":"10.1016\/j.bioorg.2025.108273_bb0595","doi-asserted-by":"crossref","first-page":"1183","DOI":"10.3390\/molecules25051183","article-title":"1,2,4-Triazolo[1,5-a]pyrimidines as a novel class of inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H activity","volume":"25","author":"Desantis","year":"2020","journal-title":"Molecules"},{"key":"10.1016\/j.bioorg.2025.108273_bb0600","doi-asserted-by":"crossref","first-page":"13658","DOI":"10.1021\/acs.jmedchem.1c01015","article-title":"Discovery of novel dihydrothiopyrano[4,3-d]pyrimidine derivatives as potent HIV-1 NNRTIs with significantly reduced hERG inhibitory activity and improved resistance profiles","volume":"64","author":"Wang","year":"2021","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0605","doi-asserted-by":"crossref","first-page":"1298","DOI":"10.1021\/acs.jmedchem.9b01769","article-title":"Discovery and characterization of fluorine-substituted Diarylpyrimidine derivatives as novel HIV-1 NNRTIs with highly improved resistance profiles and low activity for the hERG Ion Channel","volume":"63","author":"Kang","year":"2020","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0610","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.112811","article-title":"Targeting dual tolerant regions of binding pocket: discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility","volume":"206","author":"Wang","year":"2020","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0615","doi-asserted-by":"crossref","first-page":"1484","DOI":"10.1021\/acs.jmedchem.8b01656","article-title":"Identification of Dihydrofuro[3,4- d]pyrimidine derivatives as novel HIV-1 non-nucleoside reverse transcriptase inhibitors with promising antiviral activities and desirable physicochemical properties","volume":"62","author":"Kang","year":"2019","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0620","doi-asserted-by":"crossref","first-page":"878","DOI":"10.1016\/j.apsb.2019.08.013","article-title":"Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs","volume":"10","author":"Kang","year":"2020","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.bioorg.2025.108273_bb0625","doi-asserted-by":"crossref","DOI":"10.1016\/j.bioorg.2019.102974","article-title":"Follow on-based optimization of the biphenyl-DAPYs as HIV-1 nonnucleoside reverse transcriptase inhibitors against the wild-type and mutant strains","volume":"89","author":"Sang","year":"2019","journal-title":"Bioorg. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0630","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2019.111603","article-title":"Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"182","author":"Sang","year":"2019","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0635","doi-asserted-by":"crossref","first-page":"2009","DOI":"10.1111\/cbdd.13373","article-title":"Design, synthesis, and antiviral evaluation of novel hydrazone-substituted thiophene[3,2-d]pyrimidine derivatives as potent human immunodeficiency virus-1 inhibitors","volume":"92","author":"Wang","year":"2018","journal-title":"Chem. Biol. Drug Des."},{"key":"10.1016\/j.bioorg.2025.108273_bb0640","doi-asserted-by":"crossref","first-page":"430","DOI":"10.1111\/cbdd.13429","article-title":"Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors by exploring the structure-activity relationship of solvent-exposed regions I","volume":"93","author":"Kang","year":"2019","journal-title":"Chem. Biol. Drug Des."},{"key":"10.1016\/j.bioorg.2025.108273_bb0645","doi-asserted-by":"crossref","first-page":"1188","DOI":"10.1021\/acsmedchemlett.7b00361","article-title":"Discovery of Thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs targeting the tolerant region I of NNIBP","volume":"8","author":"Kang","year":"2017","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0650","doi-asserted-by":"crossref","first-page":"4424","DOI":"10.1021\/acs.jmedchem.7b00332","article-title":"Structure-based optimization of Thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with improved potency against resistance-associated variants","volume":"60","author":"Kang","year":"2017","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0655","article-title":"Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket","volume":"214","author":"Sun","year":"2011","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0660","doi-asserted-by":"crossref","first-page":"787","DOI":"10.1021\/acsinfecdis.9b00229","article-title":"Molecular hybridization-inspired optimization of diarylbenzopyrimidines as HIV-1 nonnucleoside reverse transcriptase inhibitors with improved activity against K103N and E138K mutants and pharmacokinetic profiles","volume":"6","author":"Han","year":"2020","journal-title":"ACS Infec. Dis."},{"key":"10.1016\/j.bioorg.2025.108273_bb0665","doi-asserted-by":"crossref","first-page":"764","DOI":"10.1016\/j.cclet.2019.11.020","article-title":"Fragment-based discovery of sulfur-containing diarylbenzopyrimidines as novel nonnucleoside reverse transcriptase inhibitors","volume":"31","author":"Han","year":"2020","journal-title":"Chin. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0670","doi-asserted-by":"crossref","first-page":"74","DOI":"10.1038\/s42004-019-0174-8","article-title":"Discovery of piperidine-substituted thiazolo[5,4-d]pyrimidine derivatives as potent and orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"2","author":"Kang","year":"2019","journal-title":"Commun. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0675","doi-asserted-by":"crossref","first-page":"11","DOI":"10.1016\/j.ejmech.2019.05.011","article-title":"Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains","volume":"176","author":"Jin","year":"2019","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0680","doi-asserted-by":"crossref","first-page":"149","DOI":"10.1016\/j.ejmech.2017.09.054","article-title":"Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H","volume":"141","author":"Kankanala","year":"2017","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0685","series-title":"Fused Pyrimidine Compounds for the Treatment of HIV","author":"Jansa","year":"2016"},{"key":"10.1016\/j.bioorg.2025.108273_bb0690","series-title":"Isoquinoline Compounds for the Treatment of HIV","author":"Jansa","year":"2016"},{"key":"10.1016\/j.bioorg.2025.108273_bb0695","series-title":"Quinazoline Derivatives Used to Treat HIV","author":"Jansa","year":"2016"},{"issue":"2017","key":"10.1016\/j.bioorg.2025.108273_bb0700","doi-asserted-by":"crossref","first-page":"383","DOI":"10.1080\/13543776.2017.1303046","article-title":"Novel fused pyrimidine and isoquinoline derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2016105532A1, WO2016105534A1 and WO2016105564A1","volume":"27","author":"Kang","year":"2017","journal-title":"Exp. Opin. Therap Pat."},{"key":"10.1016\/j.bioorg.2025.108273_bb0705","doi-asserted-by":"crossref","first-page":"4053","DOI":"10.1016\/j.cclet.2021.02.033","article-title":"Boronic acid-containing diarylpyrimidine derivatives as novel HIV-1 NNRTIs: design, synthesis and biological evaluation","volume":"32","author":"Feng","year":"2021","journal-title":"Chin. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0710","doi-asserted-by":"crossref","first-page":"1215","DOI":"10.3390\/ijms24021215","article-title":"Covalently targeted highly conserved Tyr318 to improve the drug resistance profiles of HIV-1 NNRTIs: a proof-of-concept study","volume":"24","author":"Zhou","year":"2023","journal-title":"Int. J. Mol. Sci."},{"key":"10.1016\/j.bioorg.2025.108273_bb0715","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmc.2023.117484","article-title":"In situ click chemistry-based discovery of 1,2,3-triazole-derived diarylpyrimidines as novel HIV-1 NNRTIs by exploiting the tolerant region I in binding pocket","volume":"96","author":"Sun","year":"2023","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0720","doi-asserted-by":"crossref","first-page":"8643","DOI":"10.1021\/acs.jmedchem.3c00275","volume":"66","author":"Wang","year":"2023","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0725","doi-asserted-by":"crossref","first-page":"1257","DOI":"10.1016\/j.apsb.2023.11.023","article-title":"Structure-based design and optimization lead to the identification of novel dihydrothiopyrano[3,2-d]pyrimidine derivatives as potent HIV-1 inhibitors against drug-resistant varians","volume":"14","author":"Wang","year":"2024","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.bioorg.2025.108273_bb0730","doi-asserted-by":"crossref","first-page":"3110","DOI":"10.1016\/j.apsb.2024.03.021","article-title":"Design and optimization of piperidine-substituted thiophene[3,2-d]pyrimidine-based HIV-1 NNRTIs with improved drug resistance and pharmacokinetic profiles","volume":"14","author":"Sun","year":"2024","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.bioorg.2025.108273_bb0735","doi-asserted-by":"crossref","DOI":"10.1016\/j.cclet.2023.108827","article-title":"Design, synthesis, and biological evaluation of benzo[4,5]thieno[2,3-d]pyrimidine derivatives as novel HIV-1 NNRTIs","volume":"35","author":"Meng","year":"2024","journal-title":"Chin. Chem. Lett."},{"key":"10.1016\/j.bioorg.2025.108273_bb0740","article-title":"Current development of 1, 2, 3-triazole derived potential antimalarial scaffolds: structure activity relationship (SAR) and bioactive compounds","volume":"115699","author":"Rahman","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0745","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2024.117033","article-title":"Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile","volume":"281","author":"Dai","year":"2025","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.bioorg.2025.108273_bb0750","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2024.116941","article-title":"Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses","volume":"280","author":"Jiang","year":"2024","journal-title":"Eur. J. Med. Chem."}],"container-title":["Bioorganic Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0045206825001531?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0045206825001531?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,11,22]],"date-time":"2025-11-22T21:38:57Z","timestamp":1763847537000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0045206825001531"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,4]]},"references-count":150,"alternative-id":["S0045206825001531"],"URL":"https:\/\/doi.org\/10.1016\/j.bioorg.2025.108273","relation":{},"ISSN":["0045-2068"],"issn-type":[{"value":"0045-2068","type":"print"}],"subject":[],"published":{"date-parts":[[2025,4]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Recent developments of pyrimidine appended HIV-1 non-nucleoside reverse transcriptase inhibitors","name":"articletitle","label":"Article Title"},{"value":"Bioorganic Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bioorg.2025.108273","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Elsevier Inc. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"108273"}}