麻疹病毒RNA依赖性RNA聚合酶复合物活性的非核苷抑制剂：合成与体外评价。
Non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex activity: Synthesis and in vitro evaluation.
作者信息
Sun Aiming, Chandrakumar Nizal, Yoon Jeong-Joong, Plemper Richard K, Snyder James P
机构信息
Department of Chemistry, 1515 Dickey Drive, Emory University, Atlanta, GA 30322, USA.
出版信息
Bioorg Med Chem Lett. 2007 Sep 15;17(18):5199-203. doi: 10.1016/j.bmcl.2007.06.084. Epub 2007 Jul 4.
Abstract
High-throughput screening has identified 1-methyl-3-(trifluoromethyl)-N-[4-(pyrrolidinylsulfonyl)phenyl]-1H-pyrazole-5-carboxamide 16677 as a novel and potent (IC(50)=35-145 nM) inhibitor against multiple primary isolates of diverse measles virus (MV) genotypes currently circulating worldwide. The synthesis of 16677 and several analogs together with effects on MV replication is described. The most potent analog displays nanomolar inhibition against the MV and a selectivity ratio (CC(50)/IC(50)) of ca. 16,500.
摘要
高通量筛选已确定1-甲基-3-（三氟甲基）-N-[4-（吡咯烷基磺酰基）苯基]-1H-吡唑-5-甲酰胺16677是一种新型强效（IC(50)=35 - 145 nM）抑制剂，可抑制目前在全球流行的多种不同麻疹病毒（MV）基因型的多个原始分离株。本文描述了16677及其几种类似物的合成以及对MV复制的影响。最有效的类似物对MV显示出纳摩尔级抑制作用，选择性比（CC(50)/IC(50)）约为16,500。
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