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.
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.