{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,12]],"date-time":"2026-09-12T02:35:12Z","timestamp":1789180512547,"version":"build-2803163510"},"reference-count":38,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2024,3,1]],"date-time":"2024-03-01T00:00:00Z","timestamp":1709251200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100012659","name":"Foundation for Innovative Research Groups of the National Natural Science Foundation of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100012659","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic &amp; Medicinal Chemistry Letters"],"published-print":{"date-parts":[[2024,3]]},"DOI":"10.1016\/j.bmcl.2024.129651","type":"journal-article","created":{"date-parts":[[2024,2,9]],"date-time":"2024-02-09T11:35:53Z","timestamp":1707478553000},"page":"129651","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":6,"special_numbering":"C","title":["Rational design, synthesis and biological evaluation of novel HIV-1 protease inhibitors containing 2-phenylacetamide derivatives as P2 ligands with potent activity against DRV-Resistant HIV-1 variants"],"prefix":"10.1016","volume":"101","author":[{"given":"Sihan","family":"Meng","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yu","family":"Gao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guowei","family":"Qiang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhiwei","family":"Hu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qi","family":"Shan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Juxian","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yucheng","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jie","family":"Mou","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmcl.2024.129651_b0005","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2023.115501","article-title":"HIV-1 protease inhibitors with a P1 phosphonate modification maintain potency against drug-resistant variants by increased interactions with flap residues","volume":"257","author":"Lockbaum","year":"2023","journal-title":"European Journal of Medicinal Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0010","doi-asserted-by":"crossref","first-page":"1281","DOI":"10.1056\/NEJM199804303381808","article-title":"HIV-protease inhibitors","volume":"338","author":"Flexner","year":"1998","journal-title":"The New England Journal of Medicine"},{"key":"10.1016\/j.bmcl.2024.129651_b0015","doi-asserted-by":"crossref","DOI":"10.3390\/v13050839","article-title":"HIV Protease: Historical Perspective and Current Research","volume":"13","author":"Weber","year":"2021","journal-title":"Viruses"},{"key":"10.1016\/j.bmcl.2024.129651_b0020","volume":"23","author":"M\u00f3ty\u00e1n","year":"2022","journal-title":", Potential Resistance of SARS-CoV-2 Main Protease (mpro) against Protease Inhibitors: Lessons Learned from HIV-1 Protease. International Journal of Molecular Sciences"},{"key":"10.1016\/j.bmcl.2024.129651_b0025","doi-asserted-by":"crossref","unstructured":"Spielvogel, E.; Lee, S. K.; Zhou, S.; Lockbaum, G. J.; Henes, M.; Sondgeroth, A.; Kosovrasti, K.; Nalivaika, E. A.; Ali, A.; Yilmaz, N. K.; Schiffer, C. A.; Swanstrom, R., Selection of HIV-1 for resistance to fifth-generation protease inhibitors reveals two independent pathways to high-level resistance. eLife 2023, 12.","DOI":"10.7554\/eLife.80328"},{"key":"10.1016\/j.bmcl.2024.129651_b0030","doi-asserted-by":"crossref","DOI":"10.1016\/j.bioorg.2023.106549","article-title":"Quinolines and isoquinolines as HIV-1 inhibitors: Chemical structures, action targets, and biological activities","volume":"136","author":"Hu","year":"2023","journal-title":"Bioorganic Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0035","doi-asserted-by":"crossref","first-page":"5172","DOI":"10.1021\/acs.jmedchem.5b01697","article-title":"Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV\/AIDS","volume":"59","author":"Ghosh","year":"2016","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0040","doi-asserted-by":"crossref","first-page":"10130","DOI":"10.1021\/jm301249q","article-title":"Structure-aided design of novel inhibitors of HIV protease based on a benzodiazepine scaffold","volume":"55","author":"Schimer","year":"2012","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0045","doi-asserted-by":"crossref","first-page":"e202200058","DOI":"10.1002\/cmdc.202200058","article-title":"Design, Synthesis and X-Ray Structural Studies of Potent HIV-1 Protease Inhibitors Containing C-4 Substituted Tricyclic Hexahydro-Furofuran Derivatives as P2 Ligands","volume":"17","author":"Ghosh","year":"2022","journal-title":"ChemMedChem"},{"key":"10.1016\/j.bmcl.2024.129651_b0050","doi-asserted-by":"crossref","first-page":"6157","DOI":"10.1021\/acs.jmedchem.1c02217","article-title":"Pocket-to-Lead: Structure-Based De Novo Design of Novel Non-peptidic HIV-1 Protease Inhibitors Using the Ligand Binding Pocket as a Template","volume":"65","author":"Kojima","year":"2022","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0055","doi-asserted-by":"crossref","first-page":"316","DOI":"10.1021\/acsinfecdis.8b00336","article-title":"Structural Adaptation of Darunavir Analogues against Primary Mutations in HIV-1 Protease","volume":"5","author":"Lockbaum","year":"2019","journal-title":"ACS Infectious Diseases"},{"key":"10.1016\/j.bmcl.2024.129651_b0060","doi-asserted-by":"crossref","unstructured":"A.C. Eke A.M. Stek J. Wang et al. Darunavir Pharmacokinetics With an Increased Dose During Pregnancy Journal of Acquired Immune Deficiency Syndromes 83 (1999) 2020, 373 380.","DOI":"10.1097\/QAI.0000000000002261"},{"key":"10.1016\/j.bmcl.2024.129651_b0065","volume":"9","author":"Aoki","year":"2018","journal-title":", Mechanism of Darunavir (DRV)'s High Genetic Barrier to HIV-1 Resistance: A Key V32I Substitution in Protease Rarely Occurs, but Once It Occurs, It Predisposes HIV-1 to Develop DRV Resistance."},{"key":"10.1016\/j.bmcl.2024.129651_b0070","doi-asserted-by":"crossref","first-page":"12234","DOI":"10.1073\/pnas.1400027111","article-title":"Dimerization of HIV-1 protease occurs through two steps relating to the mechanism of protease dimerization inhibition by darunavir","volume":"111","author":"Hayashi","year":"2014","journal-title":"PNAS"},{"key":"10.1016\/j.bmcl.2024.129651_b0075","doi-asserted-by":"crossref","first-page":"17190","DOI":"10.1074\/jbc.M701304200","article-title":"Mutational and structural studies aimed at characterizing the monomer of HIV-1 protease and its precursor","volume":"282","author":"Ishima","year":"2007","journal-title":"The Journal of Biological Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0080","doi-asserted-by":"crossref","first-page":"56","DOI":"10.1016\/j.coviro.2021.09.009","article-title":"Drug resistance mutations in HIV: new bioinformatics approaches and challenges","volume":"51","author":"Blassel","year":"2021","journal-title":"Current Opinion in Virology"},{"key":"10.1016\/j.bmcl.2024.129651_b0085","doi-asserted-by":"crossref","DOI":"10.3390\/v15010107","article-title":"The Effect of Treatment-Associated Mutations on HIV Replication and Transmission Cycles","volume":"15","author":"Johnson","year":"2022","journal-title":"Viruses"},{"key":"10.1016\/j.bmcl.2024.129651_b0090","doi-asserted-by":"crossref","first-page":"1058","DOI":"10.1093\/cid\/cir093","article-title":"Assessments of HIV drug resistance mutations in resource-limited settings","volume":"52","author":"Jordan","year":"2011","journal-title":"Clinical Infectious Diseases"},{"key":"10.1016\/j.bmcl.2024.129651_b0095","doi-asserted-by":"crossref","DOI":"10.1128\/mBio.02036-20","article-title":"In Vivo Emergence of a Novel Protease Inhibitor Resistance Signature in HIV-1 Matrix","volume":"11","author":"Datir","year":"2020","journal-title":"MBio"},{"key":"10.1016\/j.bmcl.2024.129651_b0100","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2019.111866","article-title":"Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV-1 variants","volume":"185","author":"Zhu","year":"2020","journal-title":"European Journal of Medicinal Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0105","doi-asserted-by":"crossref","first-page":"1786","DOI":"10.1021\/ct300032r","article-title":"How Does Darunavir Prevent HIV-1 Protease Dimerization?","volume":"8","author":"Huang","year":"2012","journal-title":"Journal of Chemical Theory and Computation"},{"key":"10.1016\/j.bmcl.2024.129651_b0110","doi-asserted-by":"crossref","first-page":"1189","DOI":"10.1080\/13543784.2016.1212837","article-title":"Investigational protease inhibitors as antiretroviral therapies","volume":"25","author":"Midde","year":"2016","journal-title":"Expert Opinion on Investigational Drugs"},{"key":"10.1016\/j.bmcl.2024.129651_b0115","doi-asserted-by":"crossref","first-page":"6470","DOI":"10.1021\/jacs.1c00016","article-title":"Backbone Modifications of HLA-A2-Restricted Antigens Induce Diverse Binding and T Cell Activation Outcomes","volume":"143","author":"Gibadullin","year":"2021","journal-title":"Journal of the American Chemical Society"},{"key":"10.1016\/j.bmcl.2024.129651_b0120","doi-asserted-by":"crossref","first-page":"236","DOI":"10.1016\/j.molimm.2013.07.014","article-title":"Selectivity of binding of PEGs and PEG-like oligomers to anti-PEG antibodies induced by methoxyPEG-proteins","volume":"57","author":"Saifer","year":"2014","journal-title":"Molecular Immunology"},{"key":"10.1016\/j.bmcl.2024.129651_b0125","doi-asserted-by":"crossref","first-page":"1863","DOI":"10.1002\/cmdc.201900508","article-title":"Potent HIV-1 Protease Inhibitors Containing Carboxylic and Boronic Acids: Effect on Enzyme Inhibition and Antiviral Activity and Protein-Ligand X-ray Structural Studies","volume":"14","author":"Ghosh","year":"2019","journal-title":"ChemMedChem"},{"key":"10.1016\/j.bmcl.2024.129651_b0130","doi-asserted-by":"crossref","first-page":"13","DOI":"10.1186\/s12977-020-00520-6","article-title":"Non-active site mutants of HIV-1 protease influence resistance and sensitisation towards protease inhibitors","volume":"17","author":"Bastys","year":"2020","journal-title":"Retrovirology"},{"key":"10.1016\/j.bmcl.2024.129651_b0135","doi-asserted-by":"crossref","first-page":"2913","DOI":"10.1038\/s41598-022-07012-x","article-title":"Prediction and molecular field view of drug resistance in HIV-1 protease mutants","volume":"12","author":"Wang","year":"2022","journal-title":"Scientific Reports"},{"key":"10.1016\/j.bmcl.2024.129651_b0140","doi-asserted-by":"crossref","first-page":"1055","DOI":"10.1093\/cid\/ciab583","article-title":"Transmitted Drug Resistance Among Human Immunodeficiency Virus (HIV)-1 Diagnoses in the United States, 2014\u20132018","volume":"74","author":"McClung","year":"2022","journal-title":"Clinical Infectious Diseases"},{"key":"10.1016\/j.bmcl.2024.129651_b0145","doi-asserted-by":"crossref","first-page":"974","DOI":"10.1016\/j.bbrc.2019.05.064","article-title":"Structural studies of antiviral inhibitor with HIV-1 protease bearing drug resistant substitutions of V32I, I47V and V82I","volume":"514","author":"Pawar","year":"2019","journal-title":"Biochemical and Biophysical Research Communications"},{"key":"10.1016\/j.bmcl.2024.129651_b0150","doi-asserted-by":"crossref","first-page":"e28184","DOI":"10.1002\/jmv.28184","article-title":"Prevalence of drug resistant HIV-1 forms in patients without any history of antiretroviral therapy in the Republic of Guinea","volume":"95","author":"Shchemelev","year":"2023","journal-title":"Journal of Medical Virology"},{"key":"10.1016\/j.bmcl.2024.129651_b0155","doi-asserted-by":"crossref","first-page":"69","DOI":"10.1186\/s12906-020-2816-x","article-title":"In vitro anti-HIV activity of some Indian medicinal plant extracts","volume":"20","author":"Palshetkar","year":"2020","journal-title":"BMC Complementary Medicine and Therapies"},{"key":"10.1016\/j.bmcl.2024.129651_b0160","doi-asserted-by":"crossref","DOI":"10.1128\/AAC.00372-19","volume":"63","author":"Takamatsu","year":"2019","journal-title":"Antimicrobial Agents and Chemotherapy"},{"key":"10.1016\/j.bmcl.2024.129651_b0165","doi-asserted-by":"crossref","first-page":"355","DOI":"10.1021\/ml500533x","article-title":"Phenolic diterpenoid derivatives as anti-influenza a virus agents","volume":"6","author":"Dang","year":"2015","journal-title":"ACS Medicinal Chemistry Letters"},{"key":"10.1016\/j.bmcl.2024.129651_b0170","doi-asserted-by":"crossref","first-page":"223","DOI":"10.1016\/S1387-2656(07)13009-X","article-title":"Potentials of phenolic molecules of natural origin and their derivatives as anti-HIV agents","volume":"13","author":"Hassan Khan","year":"2007","journal-title":"Biotechnology Annual Review"},{"key":"10.1016\/j.bmcl.2024.129651_b0175","doi-asserted-by":"crossref","DOI":"10.1016\/j.bcp.2023.115495","article-title":"Phenolic compound SG-1 from Balanophora harlandii and its derivatives exert anti-influenza A virus activity via activation of the Nrf2\/HO-1 pathway","volume":"210","author":"Zhou","year":"2023","journal-title":"Biochemical Pharmacology"},{"key":"10.1016\/j.bmcl.2024.129651_b0180","first-page":"954","volume":"247","author":"Matayoshi","year":"1990","journal-title":"Novel Fluorogenic Substrates for Assaying Retroviral Proteases by Resonance Energy Transfer"},{"key":"10.1016\/j.bmcl.2024.129651_b0185","doi-asserted-by":"crossref","first-page":"8062","DOI":"10.1021\/acs.jmedchem.9b00838","article-title":"HIV-1 Protease Inhibitors Incorporating Stereochemically Defined P2' Ligands To Optimize Hydrogen Bonding in the Substrate Envelope","volume":"62","author":"Rusere","year":"2019","journal-title":"Journal of Medicinal Chemistry"},{"key":"10.1016\/j.bmcl.2024.129651_b0190","doi-asserted-by":"crossref","first-page":"e344","DOI":"10.1002\/hsr2.344","article-title":"HIV-1 molecular epidemiology in Bangladesh: A systematic review","volume":"4","author":"Molla","year":"2021","journal-title":"Health Science Reports"}],"container-title":["Bioorganic &amp; Medicinal Chemistry Letters"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X24000532?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X24000532?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,18]],"date-time":"2025-10-18T07:49:32Z","timestamp":1760773772000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0960894X24000532"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,3]]},"references-count":38,"alternative-id":["S0960894X24000532"],"URL":"https:\/\/doi.org\/10.1016\/j.bmcl.2024.129651","relation":{},"ISSN":["0960-894X"],"issn-type":[{"value":"0960-894X","type":"print"}],"subject":[],"published":{"date-parts":[[2024,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Rational design, synthesis and biological evaluation of novel HIV-1 protease inhibitors containing 2-phenylacetamide derivatives as P2 ligands with potent activity against DRV-Resistant HIV-1 variants","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry Letters","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmcl.2024.129651","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2024 Elsevier Ltd. All rights reserved.","name":"copyright","label":"Copyright"}],"article-number":"129651"}}