Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.

ID: ALA1139926

Journal: Bioorg Med Chem Lett

Title: Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.

Authors: Tanaka T, Muto T, Maruoka H, Imajo S, Fukami H, Tomimori Y, Fukuda Y, Nakatsuka T.

Abstract: A novel series of 6-substituted 4-sulfonyl-1,4-diazepane-2,5-diones were designed, synthesized and evaluated as human chymase inhibitors. Structure-activity relationship studies led to the identification of a potent inhibitor, (6S)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione, with an IC(50) of 0.027 microM.

CiteXplore: 17419055

DOI: 10.1016/j.bmcl.2007.03.038

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