Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: Further optimization of anti-hepatitis C virus activity

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• 作者：Gerhard Puerstinger ; Jan Paeshuyse ; Susanne Heinrich ; Joachim Mohr ; Nicole Schraffl ; Erik De Clercq ; Johan Neyts
• 关键词：Imidazo[4 ; 5-c]pyridines ; BVDV inhibitor ; HCV inhibitor ; Antiviral
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 September 2007
• 卷：17
• 期：18
• 页码：5111-5114
• 文件大小：121 K

摘要

Substituted 5-benzyl-2-phenyl-5H-imidazo[4,5-c]pyridines represent a novel class of compounds with activity against pestiviruses and the hepatitis C virus (HCV). Several series of analogues with modifications of the substituents in positions 2 and 5 were prepared. These efforts resulted in the discovery of several compounds with potent antiviral activity of which 2-(2,3-difluorophenyl)-5-[4-(trifluoromethyl)benzyl]-5H-imidazo[4,5-c]pyridine (46) was most potent against HCV (EC₅₀ of 0.10 μM and a selectivity index of 1080).