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

  • Bioorg Med Chem Lett. 2006 Sep 1;16(17):4444-9. doi: 10.1016/j.bmcl.2006.06.048.
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
  • 1. Valeant Research & Development, Costa Mesa, CA 92626, USA.
PMID: 16806925 DOI: 10.1016/j.bmcl.2006.06.048
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.