Synthesis and Evaluation of Pyrrolin-2-one Compounds, a Series of Plasminogen Activator Inhibitor-1 Inhibitors

Hiroshi Miyazaki; Tsuyoshi Ogiku; Hiroshi Sai; Yasunori Moritani; Akio Ohtani; Hiroshi Ohmizu

doi:10.1248/cpb.57.979

Regular Articles

Synthesis and Evaluation of Pyrrolin-2-one Compounds, a Series of Plasminogen Activator Inhibitor-1 Inhibitors

Hiroshi Miyazaki, Tsuyoshi Ogiku, Hiroshi Sai, Yasunori Moritani, Akio Ohtani, Hiroshi Ohmizu

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Keywords: plasminogen activator inhibitor-1, inhibitor, antithrombotic drug, furan-2-one, pyrrolin-2-one

JOURNAL FREE ACCESS

2009 Volume 57 Issue 9 Pages 979-985

DOI https://doi.org/10.1248/cpb.57.979

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Abstract

A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PAI-1 over other enzymes and high antithrombotic activity.

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