Synthesis of prolyl endopeptidase inhibitors and evaluation of their structure-activity relationships: In vitro inhibition of prolyl endopeptidase from canine brain

DOI: 10.1248/cpb.41.1583

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1583 - 1588 (1993)

Update date:2022-09-26

Topics: Synthesis Inhibitors In vitro Structure-activity relationships Prolyl endopeptidase

Authors:

Arai Arai

Nishioka

Niwa Niwa

Yamanaka

Tanaka Tanaka

Yoshinaga

Kobayashi

Miura Miura

Ikeda Ikeda

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Article abstract of DOI:10.1248/cpb.41.1583

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.

Full text of DOI:10.1248/cpb.41.1583

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