Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase

…, E Gunic, C Jenket, U Boyle, Y Koh, I Korboukh…

Index: De La Rosa, Martha; Kim, Hong Woo; Gunic, Esmir; Jenket, Cheryl; Boyle, Uyen; Koh, Yung-hyo; Korboukh, Ilia; Allan, Matthew; Zhang, Weijian; Chen, Huanming; Xu, Wen; Nilar, Shahul; Yao, Nanhua; Hamatake, Robert; Lang, Stanley A.; Hong, Zhi; Zhang, Zhijun; Girardet, Jean-Luc Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 17 p. 4444 - 4449

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Citation Number: 93

Abstract

A new series of 1, 2, 4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz-and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the ...