STUDIES ON ANTIPLATELET AGENTS .1. SYNTHESIS AND PLATELET INHIBITORY ACTIVITY OF 5-ALKYL-2-ARYL-4-PYRIDYLIMIDAZOLES

被引：9

作者：

TANAKA, A

ITO, K

NISHINO, S

MOTOYAMA, Y

TAKASUGI, H

机构：

[1] New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd, Osaka 532, 2-1-6 Kashima, Yodogawa-ku

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 1992年 / 40卷 / 12期

关键词：

PLATELET AGGREGATION INHIBITOR; VASORELAXANT ACTIVITY; ENZYME ACTIVITY; 5-ALKYL-2-ARYL-4-PYRIDYLIMIDAZOLE; ACUTE TOXICITY; ULCEROGENICITY;

D O I：

10.1248/cpb.40.3206

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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.

引用

页码：3206 / 3213

页数：8

共 19 条

[1]

ASSAY OF ADENOSINE 3',5'-CYCLIC MONOPHOSPHATE AND GUANOSINE 3',5'-CYCLIC MONOPHOSPHATE IN BIOLOGICAL MATERIALS BY ENZYMATIC RADIOISOTOPIC DISPLACEMENT [J].