Department of Chemistry, Boehringer Ingelheim Canada Ltd, Research and Development, 2100 Cunard Street, Laval, Québec, Canada H7S 2G5.
Bioorg Med Chem Lett. 2010 Feb 1;20(3):857-61. doi: 10.1016/j.bmcl.2009.12.101. Epub 2010 Jan 4.
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.
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。