Structure–Activity relationship of benzo [b] thiophene-2-sulfonamide derivatives as novel human chymase inhibitors

…, A Murakami, Y Koide, S Satoh, A Takahashi

文献索引：Masaki, Hidekazu; Mizuno, Yusuke; Tatui, Akira; Murakami, Akira; Koide, Yuuki; Satoh, Shoji; Takahashi, Atsuo Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 22 p. 4085 - 4088

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被引用次数: 25

摘要

We have identified a new class of chymase inhibitor through a substituent analysis of MWP00965, which we previously discovered by in silico screening. TY-51076 (7) showed high potency (IC50= 56 nM) and excellent selectivity for chymase compared to chymotrypsin and cathepsin G (> 400-fold). The synthesis and structure–activity relationship of this class are described.