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
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.
Liu, Bin,Lee, Younghee,Zou, Jinming,Petrassi, H. Michael,Joseph, Rhoda W.,Chao, Wenchun,Michelotti, Enrique L.,Bukhtiyarova, Marina,Springman, Eric B.,Dorsey, Bruce D.
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p. 6592 - 6596
(2010/12/20)
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