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Title: Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. Author: Aoyama Y, Uenaka M, Konoike T, Hayasaki-Kajiwara Y, Naya N, Nakajima M. Journal: Bioorg Med Chem Lett; 2001 Jul 09; 11(13):1691-4. PubMed ID: 11425539. 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.[Abstract] [Full Text] [Related] [New Search]