Phenyldihydroxypyrimidines as HCVNS5B RNA dependent RNA polymerase inhibitors. Part 1: Amides and ureas

被引：9

作者：

Crescenzi, B ^{[1
]}

Poma, M ^{[1
]}

Ontoria, JM ^{[1
]}

Marchetti, A ^{[1
]}

Nizi, E ^{[1
]}

Matassa, VG ^{[1
]}

Gardelli, C ^{[1
]}

机构：

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

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2005年 / 2卷 / 06期

关键词：

HCVNS5B RNA polymerase; dihydroxypyrimidines; SAR; inhibitors; amides; ureas;

D O I：

10.2174/1570180054771491

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Phenyl-5,6-dihydroxypyrimidine-4-carboxylic acids were discovered as specific inhibitors of the NS5B polymerase of the Hepatitis C Virus. In-depth structure-activity investigations at the ortho and meta positions of the phenyl ring were undertaken, and compounds with greatly improved activity over the original lead have been discovered.

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页码：451 / 455

页数：5

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