Synthesis and SAR of piperazinyl-N-phenylbenzamides as inhibitors of hepatitis C virus RNA replication in cell culture

被引：35

作者：

Conte, Immacolata ^{[1
]}

Giuliano, Claudio ^{[1
]}

Ercolani, Caterina ^{[1
]}

Narjes, Frank ^{[1
]}

Koch, Uwe ^{[2
]}

Rowley, Michael ^{[1
]}

Altamura, Sergio ^{[3
]}

De Francesco, Raffaele ^{[4
]}

Neddermann, Petra ^{[5
]}

Migliaccio, Giovanni ^{[3
]}

Stansfield, Ian ^{[1
]}

机构：

[1] Ist Ric Biol Mol P Angeletti SpA, Merck Res Labs Rome, Dept Med Chem, I-00040 Pomezia, Italy

[2] Ist Ric Biol Mol P Angeletti SpA, Merck Res Labs Rome, Dept Computat Sci, I-00040 Pomezia, Italy

[3] Ist Ric Biol Mol P Angeletti SpA, Merck Res Labs Rome, Dept Pharmacol, I-00040 Pomezia, Italy

[4] INGM, Ist Nazl Genet Mol, Dept Mol Biol & Genom, I-20122 Milan, Italy

[5] Ist Ric Biol Mol P Angeletti SpA, Merck Res Labs Rome, Dept Biochem & Cell Biol, I-00040 Pomezia, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 06期

关键词：

Hepatitis C virus; Modulation of the dimerization of NS5A; Substituted piperazinyl-N-(aryl)benzamides; PROTEIN; INTERFERON; RESISTANCE; PKR;

D O I：

10.1016/j.bmcl.2009.01.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The RNA replication machinery of HCV is a multi-subunit membrane-associated complex. NS5A has emerged as an active component of HCV replicase, possibly involved in regulation of viral replication and resistance to the antiviral effect of interferon. We report here substituted piperazinyl-N-(aryl)benzamides as potent inhibitors of HCV replication exerted via modulation of the dimerization of NS5A. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1779 / 1783

页数：5

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