Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1

  • Bioorg Med Chem Lett. 2010 Nov 15;20(22):6592-6. doi: 10.1016/j.bmcl.2010.09.034.
Bin Liu  1 ,  Younghee Lee ,  Jinming Zou ,  H Michael Petrassi ,  Rhoda W Joseph ,  Wenchun Chao ,  Enrique L Michelotti ,  Marina Bukhtiyarova ,  Eric B Springman ,  Bruce D Dorsey
Affiliations
  • 1. Ansaris, Four Valley Square, 512 E. Township Line Rd, Blue Bell, PA 19422, United States. [email protected]
PMID: 20888224 DOI: 10.1016/j.bmcl.2010.09.034
Abstract

The discovery and SAR study of a series of 4,6-diamino-1,3,5-triazin-2-ol compounds as novel HIV-1 non-nucleoside Reverse Transcriptase inhibitors (NNRTIs) are reported. The lead compounds in this series showed excellent activity against wild-type and drug-resistant RT Enzymes and viral strains. In addition, compounds from this series demonstrated favorable pharmacokinetic profile in rat. A preliminary modeling study was conducted to understand the binding mode of this series of compounds.