Arylazolylthioacetanilide. Part 11: Design, Synthesis and Biological Evaluation of 1,2,4-Triazole Thioacetanilide Derivatives as Novel Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors.


A series of novel 1,2,4-triazole thioacetanilide derivatives have 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.




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