Tanaka A, Ito K, Nishino S, Motoyama Y, Takasugi H
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1992 Dec;40(12):3206-13. 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.
合成了5-烷基-2-芳基-4-吡啶基咪唑并在大鼠离体血小板聚集研究中进行了测试。在这些化合物中，2-(2-氟苯基)-5-甲基-4-(3-吡啶基)咪唑(25)活性最强，口服剂量为10mg/kg时显示出98%的抑制率。25对环氧化酶、血栓素A2(TXA2)合成酶和磷酸二酯酶具有抑制活性，并且还显示出抑制氯化钾诱导的大鼠主动脉收缩。所有化合物几乎没有急性毒性，并且似乎对胃没有不良影响。
