摘要
对３２个（Ｅ）－１－取代芳基－２－（１Ｈ－苯并咪唑－１－基）乙酮取代苯腙类化合物初步体外药理测试结果表明，均有不同程度抑制ＴＸＡ２合成酶从而抑制花生四烯酸（ＡＡ）诱导的血小板聚集作用。化合物（２）活性最强，其活性以ＩＣ５０值相比，强于Ｄａｚｏｘｉｂｅｎ，化合物（３），（９），（１５），（２５）也有较强的抑酶活性。初步探讨了该类化合物构效关系。
Results of preliminary pharmacological tests showed that all of the test compounds had activity against TXA2 synthetase,thus inhibiting platelet aggregation induced by AA in vitro with rabbits. Compound (2) was the most potent. Its activity was stronger than that of Dazoxiben in comparison with that of IC50. Compounds (3),(9),(15),(25) also had good activity. the change of group substitution on benzene would affect inhibitory activity to TXA2 synthetase.
出处
《中国药物化学杂志》
CAS
CSCD
1995年第1期6-9,17,共5页
Chinese Journal of Medicinal Chemistry
