标题:Arylazolylthioacetanilide. Part 11: Design, synthesis and biological evaluation of 1,2,4-triazole thioacetanilide derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
作者:Li,Z.;Cao,Y.;Zhan,P.;Pannecouque,C.;Balzarini,J.;DeClercq,E.;Shen,Y.;Liu,X.
作者机构:[Li, Z] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, China;[ Cao, Y] 更多
通讯作者:Liu, XY
通讯作者地址:[Liu, XY]Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, 44 Wenhuaxi Rd, Jinan 250012, Peoples R China.
来源:Medicinal chemistry
出版年:2013
卷:9
期:7
页码:968-973
DOI:10.2174/1573406411309070010
关键词:1;2;4-triazole thioacetanilides;AIDS;Anti-HIV-1 activity;HIV-1;NNRTIs
摘要:A series of novel 1,2,4-triazole thioacetanilide derivatives has been designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. Half of these compounds showed moderate to potent activities against wild-type HIV-1 with an EC50 ranging from 38.0 μM to 4.08 μM. Among them, 2-(4-(2-fluorobenzyl)-5-isopropyl-4H-1,2,4-triazol-3-ylthio)-N-(2-nitrophenyl) acetamide 7d was identified as the most promising compound (EC50 = 4.26 μM, SI = 49). However, no compound was active against HIV-2. The preliminary structure-activity relationships among the newly synthesized congeners are discussed.
收录类别:SCOPUS;SCIE
WOS核心被引频次:6
Scopus被引频次:6
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84890263353&doi=10.2174%2f1573406411309070010&partnerID=40&md5=e3b11e3c3f883d5b0b6d84c4bc4b30ba
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