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. 2010 Nov 15;20(22):6592-6.
doi: 10.1016/j.bmcl.2010.09.034. Epub 2010 Sep 21.

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

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

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

Bin Liu et al. Bioorg Med Chem Lett. .

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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