Structure-based bioisosterism design, synthesis and biological evaluation of novel 1, 2, 4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs

…, W Chen, X Liu, C Pannecouque, E De Clercq

Index: Zhan, Peng; Li, Xiao; Li, Zhenyu; Chen, Xuwang; Tian, Ye; Chen, Wenmin; Liu, Xinyong; Pannecouque, Christophe; Clercq, Erik De Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7155 - 7162

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Citation Number: 17

Abstract

The development of new HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel chemical entities of increased potency. Previous investigations in our laboratory resulted in the discovery of several novel series of arylazolylthioacetanilides as potent NNRTIs. In this study, based on the structure-based bioisosterism strategy, novel 1, 2, 4-triazin-6-yl thioacetamide derivatives were designed, ...