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. 2010 Mar 1;20(5):1585-8.
doi: 10.1016/j.bmcl.2010.01.086. Epub 2010 Jan 21.

N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Michael L Mitchell  1 , Jong Chan Son, Ill Young Lee, Chong-Kyo Lee, Hae Soo Kim, Hongyan Guo, Jianhong Wang, Jaclyn Hayes, Michael Wang, Amber Paul, Eric B Lansdon, James M Chen, Gene Eisenberg, Romas Geleziunas, Lianhong Xu, Choung U Kim
Affiliations

N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Michael L Mitchell et al. Bioorg Med Chem Lett. .

Abstract

A series of N1-heterocyclic pyrimidinediones were extensively evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Inhibitor 1 is active against NNRTI-resistant viruses including RT mutant K103N. The co-crystal structure of inhibitor 1 with HIV-1 RT revealed that H-bonds are formed with K101 and K103. Efforts to improve the suboptimal pharmacokinetic profile of 1 resulted in the discovery of compound 13, which represents the lead compound in this series with improved pharmacokinetics and similar potency as inhibitor 1.

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