Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors

A novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones was designed, synthesized, and evaluated as human chymase inhibitors. From this series, we identified several compounds which were effective, via oral administration, in a mouse model of chronic dermatitis. A novel serie...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3435-3439
Hauptverfasser:	Maruoka, Hiroshi, Muto, Tsuyoshi, Tanaka, Taisaku, Imajo, Seiichi, Tomimori, Yoshiaki, Fukuda, Yoshiaki, Nakatsuka, Takashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Azepines - chemical synthesis Azepines - pharmacology Benzyl Compounds - chemical synthesis Benzyl Compounds - pharmacology Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Chymase Chymases - antagonists & inhibitors Dermatitis - drug therapy Dermatitis - pathology Disease Models, Animal Humans Inhibitor Inhibitory Concentration 50 Medical sciences Mice Models, Chemical Pharmacology. Drug treatments Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - pharmacology Serine Proteinase Inhibitors - therapeutic use Structure-Activity Relationship
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Zusammenfassung:	A novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones was designed, synthesized, and evaluated as human chymase inhibitors. From this series, we identified several compounds which were effective, via oral administration, in a mouse model of chronic dermatitis. A novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones was designed, synthesized, and evaluated as human chymase inhibitors. From this series, we identified several compounds which were effective, via oral administration, in a mouse model of chronic dermatitis.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.03.085