Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses
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DOI：
10.1016/j.bmcl.2013.12.070
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发表时间：
2014-02-01
影响因子：
2.7
通讯作者：
Ducharme, Yves
中科院分区：
文献类型：
--
作者：
Cote, Bernard;Burch, Jason D.;Ducharme, Yves
对一系列新的非核苷类逆转录酶抑制剂（NNRTI）进行优化，鉴定出吡酮36。在细胞培养中，这种新的NNRTI对一系列野生型和临床相关的耐药突变型HIV病毒显示出优越的效力。总体有利的临床前药代动力学特征36导致预测每天一次的低剂量人体方案。NNRTI 36，现在被称为MK-1439，目前正处于治疗HIV感染的临床开发阶段。(C) 2013 Elsevier Ltd.版权所有。
The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI) led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior potency profile against a range of wild type and clinically relevant, resistant mutant HIV viruses. The overall favorable preclinical pharmacokinetic profile of 36 led to the prediction of a once daily low dose regimen in human. NNRTI 36, now known as MK-1439, is currently in clinical development for the treatment of HIV infection. (C) 2013 Elsevier Ltd. All rights reserved.