Chemical and Pharmaceutical Bulletin p. 1583 - 1588 (1993)
Update date:2022-09-26
Topics: Synthesis Inhibitors In vitro Structure-activity relationships Prolyl endopeptidase
Arai
Nishioka
Niwa
Yamanaka
Tanaka
Yoshinaga
Kobayashi
Miura
Ikeda
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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