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N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2010
Michael L Mitchell, and
Jong Chan Son, and
Hongyan Guo, and
Yun-A Im, and
Eun Jung Cho, and
Jianhong Wang, and
Jaclyn Hayes, and
Michael Wang, and
Amber Paul, and
Eric B Lansdon, and
James M Chen, and
Doris Graupe, and
Gerry Rhodes, and
Gong-Xin He, and
Romas Geleziunas, and
Lianhong Xu, and
Choung U Kim
Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. mmitchell@gilead.com
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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