Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors |
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| Authors: | Masaki Hidekazu Mizuno Yusuke Tatui Akira Murakami Akira Koide Yuuki Satoh Shoji Takahashi Atsuo |
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| Institution: | Drug Research Department, Tokyo Research Laboratories, Toa Eiyo Ltd., 2-293-3 Amanuma-cho, Omiya-ku, Saitama-shi, Saitama 330-0834, Japan. hidekazu.masaki@toaeiyo.co.jp |
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| Abstract: | 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 (IC(50)=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. |
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