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. 2006 Sep 1;16(17):4444-9.
doi: 10.1016/j.bmcl.2006.06.048. Epub 2006 Jun 27.

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

Martha De La Rosa  1 , Hong Woo Kim, Esmir Gunic, Cheryl Jenket, Uyen Boyle, Yung-Hyo Koh, Ilia Korboukh, Matthew Allan, Weijian Zhang, Huanming Chen, Wen Xu, Shahul Nilar, Nanhua Yao, Robert Hamatake, Stanley A Lang, Zhi Hong, Zhijun Zhang, Jean-Luc Girardet
Affiliations

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

Martha De La Rosa et al. Bioorg Med Chem Lett. .

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 desired substituted anilines with thiosemicarbazones.

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