根据咪唑类和吡啶类TXA_2合成酶抑制剂的构效关系和作用机制,设计合成了20个4-{[2-(1H-咪唑基)-1-(4-取代苯基)乙氧基]甲基}苯甲酸类化合物。初步体外药理试验结果表明,所有化合物都有不同程度的抑制TXA_2合成酶能力,从而抑制花生四烯酸(AA)诱导的血小板聚集。化合物15的抑酶活性最强,以IC_(50)值相比,其活性为Dazoxiben的55.6%。并初步探讨了这类化合物的构效关系。 According to the structure-activity relationship and mechanism of TXA_2 synthetase inhibitors of imidazoles and pyridines, 20 4 - {[2- (1H-imidazolyl) -1- (4-substituted phenyl) ethoxy] Methyl} benzoic acid compounds. Preliminary in vitro pharmacological test results show that all compounds have different degrees of ability to inhibit TXA2 synthase, thereby inhibiting arachidonic acid (AA) -induced platelet aggregation. Compound 15 showed the strongest depressant activity compared to 55.6% of Dazoxiben as compared to the IC50 value. The structure-activity relationship of these compounds was also discussed.