Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(.omega.-Aminoalkoxy)phenyl]benzenes
作者:Ryoji Kikumoto、Hiroto Hara、Kunihiro Ninomiya、Masanori Osakabe、Mamoru Sugano、Harukazu Fukami、Yoshikuni Tamao
DOI:10.1021/jm00168a043
日期:1990.6
A series of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimental thrombosis in mice. The results showed that the compounds were in vitro inhibitors of collagen-induced platelet aggregation. Most of them were also effective in the mouse antithrombotic assay. The compounds
合成了一系列的[2-[(ω-氨基氨基烷氧基)苯基]乙基]苯衍生物,并评估了它们在体外抑制胶原蛋白诱导的血小板凝集和保护小鼠血栓形成的能力。结果表明该化合物是胶原诱导的血小板聚集的体外抑制剂。它们中的大多数在小鼠抗血栓形成测定中也有效。发现这些化合物是S2血清素能受体的有效拮抗剂,并且观察到它们的S2血清素能受体拮抗作用与其作为血小板抗凝剂的效力之间具有良好的相关性(r = 0.85)。在研究的化合物中,选择单[2-(二甲基氨基)-1-[[2- [2-(3-(3-甲氧基苯基)乙基]苯氧基]甲基]乙基]琥珀酸酯盐酸盐(12b,MCI-9042)进行进一步的药理和化学反应。毒理学评估。