Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase

被引：45

作者：

Ontoria, Jesus M. ^{[1
]}

Hernando, Jose I. Martin ^{[1
]}

Malancona, Savina ^{[1
]}

Attenni, Barbara ^{[1
]}

Stansfield, Ian ^{[1
]}

Conte, Immacolata ^{[1
]}

Ercolani, Caterina ^{[1
]}

Habermann, Jorg ^{[1
]}

Ponzi, Simona ^{[1
]}

Di Filippo, Marcello ^{[1
]}

Koch, Uwe ^{[1
]}

Rowley, Michael ^{[1
]}

Narjes, Frank ^{[1
]}

机构：

[1] IRBM MRL Rome, Dept Med Chem, I-00040 Pomezia, Rome, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 15期

关键词：

HCVNS5B polymerase; allosteric inhibitors; thieno[3,2-b]-pyrrole;

D O I：

10.1016/j.bmcl.2006.05.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thieno[3,2-b]pyrroles are a novel class of allosteric inhibitors of HCV NS5B RNA-dependent RNA polymerase which show potent affinity for the NS5B enzyme. Introduction of a polar substituent in the position NI led to a compound that efficiently blocks subgenomic HCV RNA replication in HUH-7 cells with an EC50 of 2.9 mu M. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4026 / 4030

页数：5

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