2. Academic Validation
  3. Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase

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

Affiliation

  • 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.

Figures