Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCVNS5B polymerase and HCV subgenomic RNA replication.: Part 2:: Tertiary amides

被引：93

作者：

Chan, L ^{[1
]}

Pereira, O ^{[1
]}

Reddy, TJ ^{[1
]}

Das, SK ^{[1
]}

Poisson, C ^{[1
]}

Courchesne, M ^{[1
]}

Proulx, M ^{[1
]}

Siddiqui, A ^{[1
]}

Yannopoulos, CG ^{[1
]}

Nguyen-Ba, N ^{[1
]}

Roy, C ^{[1
]}

Nasturica, D ^{[1
]}

Moinet, C ^{[1
]}

Bethell, R ^{[1
]}

Hamel, M ^{[1
]}

L'Heureux, L ^{[1
]}

David, M ^{[1
]}

Nicolas, O ^{[1
]}

Courtemanche-Asselin, P ^{[1
]}

Brunette, S ^{[1
]}

Bilimoria, D ^{[1
]}

Bédard, J ^{[1
]}

机构：

[1] Shire BioChem Inc, Laval, PQ H7V 4A7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

D O I：

10.1016/j.bmcl.2003.10.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

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页码：797 / 800

页数：4

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