Phenyldihydroxypyrimidines as HCVNS5B RNA dependent RNA polymerase inhibitors. Part II: Sulfonamides

被引：8

作者：

Ponzi, S ^{[1
]}

Giuliano, C ^{[1
]}

Donghi, M ^{[1
]}

Poma, M ^{[1
]}

Matassa, VG ^{[1
]}

Stansfield, I ^{[1
]}

机构：

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

来源：

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

关键词：

HCV; NS5B polymerase; inhibitors; phenyldihydroxypyrimidines; sulfonamides;

D O I：

10.2174/1570180054771527

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5,6-Dihydroxypyrimidine-4-carboxylic acids are a promising series of hepatitis C virus (HCV) NS5B polymerase inhibitors that bind at the active site of the enzyme. Here we report the evolution and SAR of a series of 2-12-[(arylsulfonyl)amino]phenyl analogues that show greater than 2 orders of magnitude improved activity over the original lead.

引用

收藏

页码：456 / 461

页数：6

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