1-Oxacephem-based human chymase inhibitors: Discovery of stable inhibitors in human plasma

被引:18
作者
Aoyama, Y [1 ]
Uenaka, M
Konoike, T
Iso, Y
Nishitani, Y
Kanda, A
Naya, N
Nakajima, M
机构
[1] Shionogi & Co Ltd, Shionogi Res Labs, Fukushima Ku, Osaka 5530002, Japan
[2] Shionogi & Co Ltd, Shionogi Res Labs, Amagasaki, Hyogo 6600813, Japan
[3] Shionogi & Co Ltd, Shionogi Res Labs, Toyonaka, Osaka 5610825, Japan
关键词
D O I
10.1016/S0960-894X(00)00489-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure-activity relationship studies of 1-oxacephems led to compounds 15, which exhibited 27 nM inhibition of human chymase and improvement of stability in human plasma (t(1/2) 1.5 h), (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2403 / 2406
页数:4
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