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ID: ALA1134118

Journal: Bioorg Med Chem Lett

Title: Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Authors: Aoyama Y, Uenaka M, Konoike T, Hayasaki-Kajiwara Y, Naya N, Nakajima M.

Abstract: The present work demonstrates that the 1,3-diazetidine-2,4-dione nucleus is effective as a scaffold of serine protease inhibitors. Compound 1 displayed high activity against human cathepsin G and alpha-chymotrypsin (0.39, 0.69 nM). Compound 6 exhibited 0.85 nM inhibition of human chymase. Compound 10 was a selective inhibitor against human neutrophil elastase.

CiteXplore: 11425539

DOI: 10.1016/s0960-894x(01)00264-5