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ID: ALA1136443

Journal: Bioorg Med Chem Lett

Title: Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.

Authors: Masaki H, Mizuno Y, Tatui A, Murakami A, Koide Y, Satoh S, Takahashi A.

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.

CiteXplore: 14592513

DOI: 10.1016/j.bmcl.2003.08.040