Solid-Phase Synthesis of Peptidomimetic Inhibitors for the Hepatitis C Virus NS3 Protease

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• 作者：Marc-André ; Poupart ; Dale R. Cameron ; Catherine Chabot ; Elise Ghiro ; Nathalie Goudreau ; Sylvie Goulet ; Martin Poirier ; and Youla S. Tsantrizos
• 刊名：Journal of Organic Chemistry
• 出版年：2001
• 出版时间：July 13, 2001
• 年：2001
• 卷：66
• 期：14
• 页码：4743 - 4751
• 全文大小：334K
• 年卷期：v.66,no.14(July 13, 2001)
• ISSN：1520-6904

文摘

The NS3 serine protease enzyme of the hepatitis C virus (HCV) is essential for viral replication.Short peptides mimicking the N-terminal substrate cleavage products of the NS3 protease are knownto act as weak inhibitors of the enzyme and have been used as templates for the design ofpeptidomimetic inhibitors. Automated solid-phase synthesis of a small library of compounds basedon such a peptidomimetic scaffold has led to the identification of potent and highly selectiveinhibitors of the NS3 protease enzyme.