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Bioorg Med Chem Lett. 2007 Jun 15;17(12):3431-4. Epub 2007 Mar 16.

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

Author information

  • 1Biomedical Research Laboratories, Daiichi Asubio Pharma Co., Ltd, 1-1-1 Wakayamadai Shimamoto-cho, Mishima-gun, Osaka 618-8513, Japan. tanaka.taisasku.fu@asubio.co.jp

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.

PMID:
17419055
[PubMed - indexed for MEDLINE]
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