68070 and CV-4151, i.e. possessing a phenyl and a heteroaryl moiety, have been prepared and found to have antiplatelet activity. The compound 2-thienyl 2'-hydroxyphenyl ketone (4) was shown to completely inhibit platelet aggregation induced by arachidonic acid at a concentration of 5.0 microM. Structure-activity analysis indicated that the presence of a ketone group is an important requirement for
R 68070和CV-4151是同时具有血栓烷合成酶抑制活性和血栓烷受体拮抗剂特性的两种化合物。已经制备了具有与R 68070和CV-4151的部分结构相似性的2-杂芳基2-取代的苯基酮衍
生物,即具有苯基和杂芳基部分,并且具有抗血小板活性。化合物2-
噻吩基2'-羟基苯基酮(4)在浓度为5.0 microM时完全抑制
花生四烯酸诱导的血小板凝集。结构活性分析表明,酮基的存在是抑制活性的重要要求。苯环上的邻羟基取代和杂芳基环的2-
噻吩基可能会增加抑制活性。