N-乙酰基吲哚羧酸类变构“指环”抑制剂对丙型肝炎病毒 NS5B 聚合酶的研究：发现与初步优化。
N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.
机构信息
Department of Chemistry, Boehringer Ingelheim Canada Ltd, Research and Development, 2100 Cunard Street, Laval, Québec, Canada H7S 2G5.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):857-61. doi: 10.1016/j.bmcl.2009.12.101. Epub 2010 Jan 4.
PMID:20074949
Abstract
SAR studies at the N(1)-position of allosteric indole-based HCV NS5B inhibitors has led to the discovery of acetamide derivatives with good cellular potency in subgenomic replicons (EC(50) <200 nM). This class of inhibitors displayed improved physicochemical properties and favorable ADME-PK profiles over previously described analogs in this class.
摘要
SAR 研究表明，变构吲哚基 HCV NS5B 抑制剂的 N(1)-位取代基，可发现具有良好细胞效力的乙酰胺衍生物，在亚基因组复制子中（EC(50) <200 nM）。与该类别的先前描述的类似物相比，这一类抑制剂具有改善的物理化学性质和有利的 ADME-PK 特征。
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