N1-烷基嘧啶二酮类作为 HIV-1 逆转录酶的非核苷抑制剂。
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
机构信息
Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1589-92. doi: 10.1016/j.bmcl.2010.01.085. Epub 2010 Jan 21.
PMID:20138513
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.
摘要
我们设计、合成并评价了一系列 N1-烷基嘧啶二酮类化合物，作为 HIV-1 非核苷逆转录酶抑制剂（NNRTIs）。我们的努力确定了化合物 10b，它是该系列的先导化合物，具有可能支持每日一次给药的药代动力学和抗病毒效力。
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