Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors

被引：56

作者：

Aoyama, Y ^{[1
]}

Uenaka, M

Kii, M

Tanaka, M

Konoike, T

Hayasaki-Kajiwara, Y

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, Osaka 5610825, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 11期

关键词：

D O I：

10.1016/S0968-0896(01)00209-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

3-Benzylazetidine-2-one derivatives were designed and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23, which exhibited 3.1 nM inhibition of human chymase and enhancement of stability in human plasma (t(1/2) 6 h). (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：3065 / 3075

页数：11

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