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ID: ALA1132518

Journal: Bioorg Med Chem Lett

Title: Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.

Authors: Iijima K, Katada J, Hayashi Y.

Abstract: We prepared a potent and relatively selective human chymase inhibitor 9 (-), based on the study of SAR of a symmetrical anhydride-type serine protease inhibitor 1. Kinetic studies suggested that 9 (-) reacts with the Ser residue at the active site of the enzyme, forming a stable acyl enzyme complex. We also showed the importance of the tri-substituted beta-amino acid structure for the potent anti-enzymatic activity.

CiteXplore: 10091694

DOI: 10.1016/s0960-894x(99)00012-8