Studies on antiplatelet agents. I. Synthesis and platelet inhibitory activity of 5-alkyl-2-aryl-4-pyridylimidazoles

DOI: 10.1248/cpb.40.3206

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 3206 - 3213 (1992)

Update date:2022-07-29

Topics:

Authors:

Tanaka Tanaka

Ito Ito

Nishino Nishino

Motoyama

Takasugi

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Article abstract of DOI:10.1248/cpb.40.3206

5-Alkyl-2-aryl-4-pyridylimidazoles were synthesized and tested in rat ex vivo platelet aggregation studies. Among these compounds, 2-(2-fluorophenyl)-5-methyl-4-(3-pyridyl)imidazole (25) was most potent, and showed 98% inhibition at a dose of 10 mg/kg (p.o.). 25 had inhibitory activity on cyclooxygenase, thromboxane A₂ (TXA₂) synthetase, and phosphodiesterase, and also showed inhibited KCl-induced contraction of rat aorta. All compounds have little acute toxicity and appear to be free of adverse effects on the stomach.

Full text of DOI:10.1248/cpb.40.3206

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