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.
Maruoka
Hiroshi
H
Biomedical Research Laboratories, Daiichi Asubio Pharma Co., Ltd, Mishima-gun, Osaka 618-8513, Japan. maruoka.hiroshi.ri@asubio.co.jp
Muto
Tsuyoshi
T
Tanaka
Taisaku
T
Imajo
Seiichi
S
Tomimori
Yoshiaki
Y
Fukuda
Yoshiaki
Y
Nakatsuka
Takashi
T
D000284:Administration, Oral; D000818:Animals; D001381:Azepines / Q000138:chemical synthesis / Q000494:pharmacology*; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D053818:Chymases / Q000037:antagonists & inhibitors*; D003872:Dermatitis / Q000188:drug therapy* / Q000473:pathology; D004195:Disease Models, Animal; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D001381:Azepines; D001593:Benzyl Compounds; D015842:Serine Proteinase Inhibitors; D053818:Chymases