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

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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. © 2006 Elsevier Ltd. All rights reserved.

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De La Rosa, M., Kim, H. W., Gunic, E., Jenket, C., Boyle, U., Koh, Y. hyo, … Girardet, J. L. (2006). Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. Bioorganic and Medicinal Chemistry Letters, 16(17), 4444–4449. https://doi.org/10.1016/j.bmcl.2006.06.048

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