2. Academic Validation
  3. Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis

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

Affiliation

  • 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.

Figures