Identification of 3-Acetyl-2-aminoquinolin-4-one as a Novel, Nonpeptidic Scaffold for Specific Calpain Inhibitory Activity

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• 作者：Da-Hye Kang ; Kyu-Yeon Jun ; Jin Pyo Lee ; Chwang Siek Pak ; Younghwa Na ; Youngjoo Kwon
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：May 14, 2009
• 年：2009
• 卷：52
• 期：9
• 页码：3093-3097
• 全文大小：121K
• 年卷期：v.52,no.9(May 14, 2009)
• ISSN：1520-4804

文摘

A series of 3-acetyl-2-aminoquinolin-4-one derivatives selected from the Korean Chemical Bank were screened for calpain inhibitory activity by using a high-throughput fluorimetric calpain assay. We identified a potent and selective μ-calpain inhibitor, compound 17, whose specificity and efficacy for μ-calpain inhibition was better than MDL28170. Docking studies revealed that the efficacy of its inhibitory effect on calpain depended on the size and charge properties of the substitutions on the phenylamino ring.