作者:Yasunori Aoyama、Masaaki Uenaka、Toshiro Konoike、Yoko Hayasaki-Kajiwara、Noriyuki Naya、Masatoshi Nakajima
DOI:10.1016/s0960-894x(01)00264-5
日期:2001.7
The present work demonstrates that the 1,3-diazetidifie-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. (C) 2001 Elsevier Science Ltd. All rights reserved.