{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T13:33:21Z","timestamp":1778679201944,"version":"3.51.4"},"reference-count":60,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2015,9,1]],"date-time":"2015-09-01T00:00:00Z","timestamp":1441065600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2015,9,1]],"date-time":"2015-09-01T00:00:00Z","timestamp":1441065600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"funder":[{"DOI":"10.13039\/501100007129","name":"Natural Science Foundation of Shandong Province","doi-asserted-by":"publisher","award":["ZR2009CM016"],"award-info":[{"award-number":["ZR2009CM016"]}],"id":[{"id":"10.13039\/501100007129","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81273354"],"award-info":[{"award-number":["81273354"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81420108027"],"award-info":[{"award-number":["81420108027"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["30910103908"],"award-info":[{"award-number":["30910103908"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100012166","name":"National Key Research and Development Program of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100012166","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100013286","name":"Specialized Research Fund for the Doctoral Program of Higher Education of China","doi-asserted-by":"publisher","award":["20110131130005"],"award-info":[{"award-number":["20110131130005"]}],"id":[{"id":"10.13039\/501100013286","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100016694","name":"Science and Technology Development Plan of Shandong Province","doi-asserted-by":"publisher","award":["2012GSF11804"],"award-info":[{"award-number":["2012GSF11804"]}],"id":[{"id":"10.13039\/100016694","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2015,9]]},"DOI":"10.1016\/j.ejmech.2015.07.043","type":"journal-article","created":{"date-parts":[[2015,7,26]],"date-time":"2015-07-26T11:02:33Z","timestamp":1437908553000},"page":"167-179","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":27,"special_numbering":"C","title":["Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors from arylthioacetanilide structural motif"],"prefix":"10.1016","volume":"102","author":[{"given":"Wenxin","family":"Li","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiao","family":"Li","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Erik","family":"De Clercq","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Peng","family":"Zhan","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xinyong","family":"Liu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"issue":"10","key":"10.1016\/j.ejmech.2015.07.043_bib1","doi-asserted-by":"crossref","first-page":"1205","DOI":"10.1097\/QAD.0b013e328354622a","article-title":"The evolving epidemiology of HIV\/AIDS","volume":"26","author":"De Cock","year":"2012","journal-title":"AIDS"},{"issue":"11","key":"10.1016\/j.ejmech.2015.07.043_bib2","doi-asserted-by":"crossref","first-page":"1083","DOI":"10.2174\/092986708784221467","article-title":"The current status of the NNRTI family of antiretrovirals used in the HAART regimen against HIV infection","volume":"15","author":"Martins","year":"2008","journal-title":"Curr. Med. Chem."},{"issue":"2","key":"10.1016\/j.ejmech.2015.07.043_bib3","doi-asserted-by":"crossref","first-page":"258","DOI":"10.1016\/S0925-4439(02)00089-3","article-title":"New developments in anti-HIV chemotherapy","volume":"1587","author":"De Clercq","year":"2002","journal-title":"BBA Mol. Basis Dis."},{"issue":"5065","key":"10.1016\/j.ejmech.2015.07.043_bib4","doi-asserted-by":"crossref","first-page":"1783","DOI":"10.1126\/science.1377403","article-title":"Crystal structure at 3.5\u00a0A resolution of HIV-1 reverse transcriptase complexed with an inhibitor","volume":"256","author":"Kohlstaedt","year":"1992","journal-title":"Science"},{"issue":"3","key":"10.1016\/j.ejmech.2015.07.043_bib5","doi-asserted-by":"crossref","first-page":"526","DOI":"10.1002\/prot.10599","article-title":"A\u00a0pharmacophore docking algorithm and its application to the cross-docking of 18 HIV-NNRTI's in their binding pockets","volume":"54","author":"Daeyaert","year":"2004","journal-title":"Proteins"},{"issue":"6","key":"10.1016\/j.ejmech.2015.07.043_bib6","doi-asserted-by":"crossref","first-page":"726","DOI":"10.1021\/jm00058a009","article-title":"Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and X-ray structure investigations","volume":"36","author":"Schaefer","year":"1993","journal-title":"J.\u00a0Med. Chem."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib7","first-page":"458","article-title":"Improving non-nucleoside reverse transcriptase inhibitors for first-line treatment of HIV infection: the development pipeline and recent clinical data","volume":"11","author":"Sweeney","year":"2008","journal-title":"Curr. Opin. Drug Discov. Devel."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib8","first-page":"110","article-title":"Emerging resistance profiles of newly approved antiretroviral drugs","volume":"16","author":"Daar","year":"2007","journal-title":"IAS-USA"},{"key":"10.1016\/j.ejmech.2015.07.043_bib9","doi-asserted-by":"crossref","first-page":"60","DOI":"10.1016\/j.ejmech.2012.02.019","article-title":"Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"51","author":"Chen","year":"2012","journal-title":"Eur. J. Med. Chem."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib10","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."},{"issue":"2","key":"10.1016\/j.ejmech.2015.07.043_bib11","doi-asserted-by":"crossref","first-page":"429","DOI":"10.1128\/AAC.01032-06","article-title":"A\u00a0novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors","volume":"51","author":"Zhang","year":"2007","journal-title":"Antimicrob. Agents Chemother."},{"issue":"8","key":"10.1016\/j.ejmech.2015.07.043_bib12","doi-asserted-by":"crossref","first-page":"3170","DOI":"10.1128\/AAC.00268-10","article-title":"Phase 2a randomized controlled trial of short-term activity, safety, and pharmacokinetics of a novel nonnucleoside reverse transcriptase inhibitor, RDEA806, in HIV-1-positive, antiretroviral-naive subjects","volume":"54","author":"Moyle","year":"2010","journal-title":"Antimicrob. Agents Chemother."},{"issue":"10","key":"10.1016\/j.ejmech.2015.07.043_bib13","doi-asserted-by":"crossref","first-page":"2748","DOI":"10.1016\/j.bmcl.2006.02.024","article-title":"Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant","volume":"16","author":"Muraglia","year":"2006","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"1","key":"10.1016\/j.ejmech.2015.07.043_bib14","doi-asserted-by":"crossref","first-page":"171","DOI":"10.1016\/j.virusres.2008.01.003","article-title":"Novel HIV-1 reverse transcriptase inhibitors","volume":"134","author":"Jochmans","year":"2008","journal-title":"Virus Res."},{"issue":"16","key":"10.1016\/j.ejmech.2015.07.043_bib15","doi-asserted-by":"crossref","first-page":"4174","DOI":"10.1016\/j.bmcl.2006.05.096","article-title":"Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"16","author":"Wang","year":"2006","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"17","key":"10.1016\/j.ejmech.2015.07.043_bib16","doi-asserted-by":"crossref","first-page":"4444","DOI":"10.1016\/j.bmcl.2006.06.048","article-title":"Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase","volume":"16","author":"De La Rosa","year":"2006","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"20","key":"10.1016\/j.ejmech.2015.07.043_bib17","first-page":"30","article-title":"Safety and pharmacokinetics of ascending single oral doses of RDEA806, a novel HIV non-nucleoside reverse transcriptase inhibitor, in healthy volunteers","volume":"10","author":"Yeh","year":"2009","journal-title":"TC"},{"key":"10.1016\/j.ejmech.2015.07.043_bib18","doi-asserted-by":"crossref","first-page":"1717","DOI":"10.1002\/cbdv.200900197","article-title":"Synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-yl]sulfanyl} acetanilides as HIV-1 inhibitors","volume":"7","author":"Zhan","year":"2010","journal-title":"Chem. Biodivers."},{"issue":"20","key":"10.1016\/j.ejmech.2015.07.043_bib19","doi-asserted-by":"crossref","first-page":"5368","DOI":"10.1016\/j.bmcl.2008.09.055","article-title":"1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"18","author":"Zhan","year":"2008","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"16","key":"10.1016\/j.ejmech.2015.07.043_bib20","doi-asserted-by":"crossref","first-page":"5775","DOI":"10.1016\/j.bmc.2009.07.028","article-title":"Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors","volume":"17","author":"Zhan","year":"2009","journal-title":"Bioorg. Med. Chem."},{"issue":"16","key":"10.1016\/j.ejmech.2015.07.043_bib21","doi-asserted-by":"crossref","first-page":"5920","DOI":"10.1016\/j.bmc.2009.07.004","article-title":"Novel 1,2,3-thiadiazole derivatives as HIV-1 NNRTIs with improved potency: synthesis and preliminary SAR studies","volume":"17","author":"Zhan","year":"2009","journal-title":"Bioorg. Med. Chem."},{"issue":"16","key":"10.1016\/j.ejmech.2015.07.043_bib22","doi-asserted-by":"crossref","first-page":"4437","DOI":"10.1016\/j.bmcl.2007.06.012","article-title":"Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N\/Y181C double mutant reverse transcriptases","volume":"17","author":"Gagnon","year":"2007","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"12","key":"10.1016\/j.ejmech.2015.07.043_bib23","doi-asserted-by":"crossref","first-page":"3326","DOI":"10.1021\/ci400427a","article-title":"Assessing molecular docking tools for relative biological activity prediction: a case study of triazole HIV-1 NNRTIs","volume":"53","author":"Fraczek","year":"2013","journal-title":"J.\u00a0Chem. Inf. Model."},{"issue":"11","key":"10.1016\/j.ejmech.2015.07.043_bib24","doi-asserted-by":"crossref","first-page":"4648","DOI":"10.1016\/j.ejmech.2009.06.037","article-title":"Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors","volume":"44","author":"Zhan","year":"2009","journal-title":"Eur. J. Med. Chem."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib25","doi-asserted-by":"crossref","first-page":"1199","DOI":"10.1016\/j.bmcl.2008.12.074","article-title":"Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N\/Y181C double mutant reverse transcriptases","volume":"19","author":"Gagnon","year":"2009","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"17","key":"10.1016\/j.ejmech.2015.07.043_bib26","doi-asserted-by":"crossref","first-page":"6374","DOI":"10.1016\/j.bmc.2009.07.027","article-title":"1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation","volume":"17","author":"Zhan","year":"2009","journal-title":"Bioorg. Med. Chem."},{"issue":"6","key":"10.1016\/j.ejmech.2015.07.043_bib27","doi-asserted-by":"crossref","first-page":"975","DOI":"10.1007\/s12272-012-0604-y","article-title":"Arylazolyl(azinyl)thioacetanilide. Part 9: synthesis and biological investigation of thiazolylthioacetamides derivatives as a novel class of potential antiviral agents","volume":"35","author":"Zhan","year":"2012","journal-title":"Arch. Pharm. Res."},{"key":"10.1016\/j.ejmech.2015.07.043_bib28","first-page":"31","article-title":"Synthesis and anti-HIV activity evaluation of 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives","author":"Jiang","year":"2012","journal-title":"Lat. Am. J. Pharm."},{"issue":"23","key":"10.1016\/j.ejmech.2015.07.043_bib29","doi-asserted-by":"crossref","first-page":"7155","DOI":"10.1016\/j.bmcl.2012.09.062","article-title":"Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs","volume":"22","author":"Zhan","year":"2012","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"5","key":"10.1016\/j.ejmech.2015.07.043_bib30","doi-asserted-by":"crossref","first-page":"810","DOI":"10.1039\/c3md00028a","article-title":"Discovery of novel pyridazinylthioacetamides as potent HIV-1 NNRTIs using a structure-based bioisosterism approach","volume":"4","author":"Song","year":"2013","journal-title":"Med. Chem. Comm."},{"issue":"23","key":"10.1016\/j.ejmech.2015.07.043_bib31","doi-asserted-by":"crossref","first-page":"6795","DOI":"10.1016\/j.bmc.2012.09.058","article-title":"Discovery of novel 2-(3-(2-chlorophenyl) pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach","volume":"20","author":"Zhan","year":"2012","journal-title":"Bioorg. Med. Chem."},{"issue":"18","key":"10.1016\/j.ejmech.2015.07.043_bib32","doi-asserted-by":"crossref","first-page":"5527","DOI":"10.1016\/j.bmc.2012.07.026","article-title":"Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors","volume":"20","author":"Li","year":"2012","journal-title":"Bioorg. Med. Chem."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib33","doi-asserted-by":"crossref","first-page":"1459","DOI":"10.1016\/j.bmc.2013.12.045","article-title":"Design and synthesis of N(1)-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"22","author":"Monforte","year":"2014","journal-title":"Bioorg. Med. Chem."},{"issue":"12","key":"10.1016\/j.ejmech.2015.07.043_bib34","doi-asserted-by":"crossref","first-page":"3362","DOI":"10.1016\/j.bmcl.2007.03.097","article-title":"Scaffold hopping in the rational design of novel HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"17","author":"O'Meara","year":"2007","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"7","key":"10.1016\/j.ejmech.2015.07.043_bib35","doi-asserted-by":"crossref","first-page":"652","DOI":"10.1007\/s00044-009-9220-x","article-title":"Synthesis and anti-HIV activity evaluation of novel N\u2032-arylidene-2-[1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio] acetohydrazides","volume":"19","author":"Zhan","year":"2010","journal-title":"Med. Chem. Res."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib36","doi-asserted-by":"crossref","first-page":"420","DOI":"10.1111\/cbdd.12328","article-title":"Synthesis and anti-HIV activity of 4-(naphthalen-1-yl)-1,2,5-thiadiazol-3-hydroxyl derivatives","volume":"84","author":"Rai","year":"2014","journal-title":"Chem. Biol. Drug Des."},{"issue":"8\u20139","key":"10.1016\/j.ejmech.2015.07.043_bib37","doi-asserted-by":"crossref","first-page":"653","DOI":"10.1023\/A:1021954728347","article-title":"A\u00a0comparison of the pharmacophore identification programs: catalyst, DISCO and GASP","volume":"16","author":"Patel","year":"2002","journal-title":"J.\u00a0Comput. Aid Mol. Des."},{"issue":"17","key":"10.1016\/j.ejmech.2015.07.043_bib38","doi-asserted-by":"crossref","first-page":"5119","DOI":"10.1016\/j.bmcl.2009.07.031","article-title":"Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants","volume":"19","author":"Su","year":"2009","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"8","key":"10.1016\/j.ejmech.2015.07.043_bib39","doi-asserted-by":"crossref","first-page":"1014","DOI":"10.2174\/138955709788681618","article-title":"Sulfanyltriazole\/tetrazoles: a promising class of HIV-1 NNRTIs","volume":"9","author":"Zhan","year":"2009","journal-title":"Mini Rev. Med. Chem."},{"issue":"20","key":"10.1016\/j.ejmech.2015.07.043_bib40","doi-asserted-by":"crossref","first-page":"6503","DOI":"10.1021\/jm800856c","article-title":"Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl) methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses","volume":"51","author":"Tucker","year":"2008","journal-title":"J.\u00a0Med. Chem."},{"issue":"23","key":"10.1016\/j.ejmech.2015.07.043_bib41","doi-asserted-by":"crossref","first-page":"7449","DOI":"10.1021\/jm800527x","article-title":"Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase","volume":"51","author":"Sweeney","year":"2008","journal-title":"J.\u00a0Med. Chem."},{"issue":"15","key":"10.1016\/j.ejmech.2015.07.043_bib42","doi-asserted-by":"crossref","first-page":"4352","DOI":"10.1016\/j.bmcl.2008.06.072","article-title":"Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase","volume":"18","author":"Sweeney","year":"2008","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"15","key":"10.1016\/j.ejmech.2015.07.043_bib43","doi-asserted-by":"crossref","first-page":"4348","DOI":"10.1016\/j.bmcl.2008.06.080","article-title":"Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase","volume":"18","author":"Sweeney","year":"2008","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"3","key":"10.1016\/j.ejmech.2015.07.043_bib44","doi-asserted-by":"crossref","first-page":"1131","DOI":"10.1016\/j.bmcl.2007.11.127","article-title":"Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase \u2013 structure\u2013activity relationships and crystallographic analysis","volume":"18","author":"Kirschberg","year":"2008","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"1","key":"10.1016\/j.ejmech.2015.07.043_bib45","doi-asserted-by":"crossref","first-page":"29","DOI":"10.2174\/092986711793979733","article-title":"Functional roles of azoles motif in anti-HIV agents","volume":"18","author":"Zhan","year":"2011","journal-title":"Curr. Med. Chem."},{"issue":"16","key":"10.1016\/j.ejmech.2015.07.043_bib46","doi-asserted-by":"crossref","first-page":"4437","DOI":"10.1016\/j.bmcl.2007.06.012","article-title":"Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N\/Y181C double mutant reverse transcriptases","volume":"17","author":"Gagnon","year":"2007","journal-title":"Bioorg. Med. Chem. Lett."},{"issue":"19","key":"10.1016\/j.ejmech.2015.07.043_bib47","doi-asserted-by":"crossref","first-page":"14316","DOI":"10.1074\/jbc.275.19.14316","article-title":"Binding of the second generation non-nucleoside inhibitor S-1153 to HIV-1 reverse transcriptase involves extensive main chain hydrogen bonding","volume":"275","author":"Ren","year":"2000","journal-title":"J.\u00a0Biol. Chem."},{"issue":"8","key":"10.1016\/j.ejmech.2015.07.043_bib48","doi-asserted-by":"crossref","first-page":"3984","DOI":"10.1073\/pnas.94.8.3984","article-title":"Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis (heteroaryl) piperazine (BHAP) U-90152 explain resistance mutations for this nonnucleoside inhibitor","volume":"94","author":"Esnouf","year":"1997","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"issue":"24","key":"10.1016\/j.ejmech.2015.07.043_bib49","doi-asserted-by":"crossref","first-page":"5912","DOI":"10.1021\/jm040071z","article-title":"Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1","volume":"47","author":"Hopkins","year":"2004","journal-title":"J.\u00a0Med. Chem."},{"issue":"8","key":"10.1016\/j.ejmech.2015.07.043_bib50","doi-asserted-by":"crossref","first-page":"1589","DOI":"10.1021\/jm960056x","article-title":"Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors","volume":"39","author":"Hopkins","year":"1996","journal-title":"J.\u00a0Med. Chem."},{"issue":"29","key":"10.1016\/j.ejmech.2015.07.043_bib51","doi-asserted-by":"crossref","first-page":"3903","DOI":"10.2174\/092986709789178019","article-title":"Design strategies of novel NNRTIs to overcome drug resistance","volume":"16","author":"Zhan","year":"2009","journal-title":"Curr. Med. Chem."},{"issue":"6","key":"10.1016\/j.ejmech.2015.07.043_bib52","doi-asserted-by":"crossref","first-page":"587","DOI":"10.2174\/138161209787315594","article-title":"Designing multiple ligands \u2013 medicinal chemistry strategies and challenges","volume":"15","author":"Morphy","year":"2009","journal-title":"Curr. Pharm. Des."},{"issue":"16","key":"10.1016\/j.ejmech.2015.07.043_bib53","doi-asserted-by":"crossref","first-page":"1893","DOI":"10.2174\/138161209788453266","article-title":"Designed multiple ligands: an emerging anti-HIV drug discovery paradigm","volume":"15","author":"Zhan","year":"2009","journal-title":"Curr. Pharm. Des."},{"key":"10.1016\/j.ejmech.2015.07.043_bib54","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."},{"issue":"9","key":"10.1016\/j.ejmech.2015.07.043_bib55","doi-asserted-by":"crossref","first-page":"3911","DOI":"10.1073\/pnas.91.9.3911","article-title":"Structure of the binding site for nonnucleoside inhibitors of the reverse transcriptase of human immunodeficiency virus type 1","volume":"91","author":"Smerdon","year":"1994","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"issue":"23","key":"10.1016\/j.ejmech.2015.07.043_bib56","doi-asserted-by":"crossref","first-page":"7153","DOI":"10.1021\/jm050257d","article-title":"Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity","volume":"48","author":"Fattorusso","year":"2005","journal-title":"J.\u00a0Med. Chem."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib57","doi-asserted-by":"crossref","first-page":"1224","DOI":"10.1021\/jm801395v","article-title":"Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations","volume":"52","author":"Butini","year":"2009","journal-title":"Eur. J. Med. Chem."},{"issue":"4","key":"10.1016\/j.ejmech.2015.07.043_bib58","doi-asserted-by":"crossref","first-page":"795","DOI":"10.1006\/jmbi.2001.4988","article-title":"Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation non-nucleoside inhibitors","volume":"312","author":"Ren","year":"2001","journal-title":"J.\u00a0Mol. Biol."},{"issue":"5","key":"10.1016\/j.ejmech.2015.07.043_bib59","doi-asserted-by":"crossref","first-page":"1466","DOI":"10.1073\/pnas.0711209105","article-title":"High-resolution structures of HIV-1 reverse transcriptase\/TMC278 complexes: strategic flexibility explains potency against resistance mutations","volume":"105","author":"Das","year":"2008","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.ejmech.2015.07.043_bib60","doi-asserted-by":"crossref","first-page":"330","DOI":"10.1016\/j.ejmech.2015.02.022","article-title":"Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines","volume":"93","author":"Huang","year":"2015","journal-title":"Eur. J. Med. Chem."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523415301756?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523415301756?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T12:51:15Z","timestamp":1778676675000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523415301756"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2015,9]]},"references-count":60,"alternative-id":["S0223523415301756"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2015.07.043","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2015,9]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors from arylthioacetanilide structural motif","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2015.07.043","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"Copyright \u00a9 2015 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}]}}