Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCVNS5B polymerase and HCV subgenomic RNA replication.: Part 2:: Tertiary amides
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCVNS5B polymerase and HCV subgenomic RNA replication.: Part 2:: Tertiary amides
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DOI：
10.1016/j.bmcl.2003.10.068
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发表时间：
2004-02-09
影响因子：
2.7
通讯作者：
Bédard, J
中科院分区：
文献类型：
--
作者：
Chan, L;Pereira, O;Bédard, J
进一步的SAR研究噻吩-2-羧酸的报告。这些研究导致了一系列叔酰胺的鉴定，这些叔酰胺显示出体外HCV NS 5 B聚合酶和Huh-7细胞中HCV亚基因组RNA复制的抑制。从建模和转移NOE（trNOE）研究的组合推导出这类分子的生物活性构象的结构见解。(C)2003爱思唯尔有限公司。保留所有权利。
Further SAR studies on the thiophene-2-carboxylic acids are reported. These studies led to the identification of a series of tertiary amides that show inhibition of both HCV NS5B polymerase in vitro and HCV subgenomic RNA replication in Huh-7 cells. Structural insights about the bioactive conformation of this class of molecules were deduced from a combination of modeling and transferred NOE (trNOE) studies. (C) 2003 Elsevier Ltd. All rights reserved.