2. Academic Validation
  3. N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

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

  • Bioorg Med Chem Lett. 2010 Mar 1;20(5):1589-92. doi: 10.1016/j.bmcl.2010.01.085.
Michael L Mitchell 1,  Jong Chan Son,  Hongyan Guo,  Yun-A Im,  Eun Jung Cho,  Jianhong Wang,  Jaclyn Hayes,  Michael Wang,  Amber Paul,  Eric B Lansdon,  James M Chen,  Doris Graupe,  Gerry Rhodes,  Gong-Xin He,  Romas Geleziunas,  Lianhong Xu,  Choung U Kim
Affiliations

Affiliation

  • 1 Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. mmitchell@gilead.com
PMID: 20138513 DOI: 10.1016/j.bmcl.2010.01.085
Abstract

A series of N1-alkyl pyrimidinediones were designed, synthesized and evaluated as HIV-1 non-nucleoside Reverse Transcriptase inhibitors (NNRTIs). Our efforts identified compound 10b, which represents the lead compound in this series with pharmacokinetics and Antiviral potency that may support once-daily dosing.

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