title: Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
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.
authors: Shionogi Research Laboratories, Shionogi & Co., Ltd., Fukushima-ku, 553-0002, Osaka, Japan. yasunori.aoyama@shionogi.co.jp
authors: Y
authors: Y
authors: Aoyama
authors: M
authors: M
authors: Uenaka
authors: T
authors: T
authors: Konoike
authors: Y
authors: Y
authors: Hayasaki-Kajiwara
authors: N
authors: N
authors: Naya
authors: M
authors: M
authors: Nakajima
mesh_terms: D001384:Azetidines / Q000737:chemistry / Q000494:pharmacology*; D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D006801:Humans; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors; D012697:Serine Endopeptidases; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013379:Substrate Specificity
chemical_list: D001384:Azetidines; D015842:Serine Proteinase Inhibitors; D002403:Cathepsins; D012697:Serine Endopeptidases; D002918:Chymotrypsin; C117608:alpha-chymotrypsin; C534094:CTSG protein, human; D056649:Cathepsin G; D019272:Leukocyte Elastase