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Bioorg Med Chem Lett. 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.

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  • 1Ansaris, Four Valley Square, 512 E. Township Line Rd, Blue Bell, PA 19422, United States.


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.

Copyright © 2010 Elsevier Ltd. All rights reserved.

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