| Literature DB >> 20137928 |
Michael L Mitchell1, 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.
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. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20137928 DOI： 10.1016/j.bmcl.2010.01.086
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823