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Bioorg Med Chem. 2001 Nov;9(11):3065-75.

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

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1
Shionogi Research Laboratories, Shionogi & Co., Ltd., Fukushima-ku, 553-0002, Osaka, Japan. yasunori.aoyama@shionogi.co.jp

Abstract

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) 6h).

PMID:
11597491
[Indexed for MEDLINE]
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