1492902-42-7Relevant articles and documents
Arylazolylthioacetanilide. Part 11: Design, synthesis and biological evaluation of 1,2,4-triazole thioacetanilide derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
Li, Zhenyu,Cao, Yuan,Zhan, Peng,Pannecouque, Christophe,Balzarini, Jan,De Clercq, Erik,Shen, Yuemao,Liu, Xinyong
, p. 968 - 973 (2014/01/06)
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.