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
  • 1. Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. [email protected]
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.