Development of tryptase inhibitors derived from thalidomide

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• 作者：Masashi Tetsuhashi ; Minoru Ishikawa ; Mariko Hashimoto ; Yuichi Hashimoto ; Hiroshi Aoyama
• 关键词：Tryptase ; Serine protease ; Thalidomide ; Phthalimide ; Inhibitor
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：15 July 2010
• 年：2010
• 卷：18
• 期：14
• 页码：5323-5338
• 全文大小：1354 K

文摘

A novel series of tryptase inhibitors with a N-phenylphthalimide skeleton structurally derived from thalidomide (1) has been developed. Structure–activity relationship studies led to a potent and selective tryptase inhibitor, 2-(4-cyanophenyl)isoindole-1,3-dione-5-yl 3-(2-aminopyridin-5-yl)propanoate (7), with the IC₅₀ value of 78 nM.