Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):1131-4. doi: 10.1016/j.bmcl.2007.11.127.
Thorsten A Kirschberg  1 ,  Mini Balakrishnan ,  Wei Huang ,  Rebecca Hluhanich ,  Nilima Kutty ,  Albert C Liclican ,  Damian J McColl ,  Neil H Squires ,  Eric B Lansdon
Affiliations
  • 1. Gilead Sciences, Department of Medicinal Chemistry, 333 Lakeside Drive, Foster City, CA 94404, USA. [email protected]
PMID: 18083512 DOI: 10.1016/j.bmcl.2007.11.127
Abstract

A series of 3,4,5-trisubstituted 1,2,4-4H triazole derivatives was synthesized and investigated for HIV-1 Reverse Transcriptase inhibition. An X-ray structure with HIV-1 RT secured the binding mode and allowed the key interactions with the enzyme to be identified.