Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. |
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| Authors: | Y Aoyama M Uenaka T Konoike Y Hayasaki-Kajiwara N Naya M Nakajima |
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| Institution: | Shionogi Research Laboratories, Shionogi & Co., Ltd., Fukushima-ku, 553-0002, Osaka, Japan. yasunori.aoyama@shionogi.co.jp |
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| 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. |
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