2. Academic Validation
  3. 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

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

Affiliation

  • 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.

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