SYNTHESIS OF PROLYL ENDOPEPTIDASE INHIBITORS AND EVALUATION OF THEIR STRUCTURE-ACTIVITY-RELATIONSHIPS - IN-VITRO INHIBITION OF PROLYL ENDOPEPTIDASE FROM CANINE BRAIN

被引：0
|
作者：
ARAI, H
NISHIOKA, H
NIWA, S
YAMANAKA, T
TANAKA, Y
YOSHINAGA, K
KOBAYASHI, N
MIURA, N
IKEDA, Y
机构：
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1993年 / 41卷 / 09期
关键词：
PROLYL ENDOPEPTIDASE; INHIBITOR; STRUCTURE ACTIVITY RELATIONSHIP; 4-PHENYLBUTANOYL DERIVATIVE; 4-(2-THIENYL)BUTANOYL DERIVATIVE;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
By chemical modification (of a known prolyl endopeptidase (PEP) inhibitor (N-[N-(4-phenylbutanoyl)-L-prolyl]pyrrolidine; SUAM-1221), several arylalkanoyl derivatives (V-1-27) were synthesized and tested for in vitro inhibitory activity towards PEP from canine brain. Among them, 4-(2-thienyl)butanoyl derivatives (V-24-27) showed more potent PEP-inhibitory activity than SUAM-1221. The structure-activity relationships of these compounds are discussed.
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页码：1583 / 1588
页数：6
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