4-取代的1-[二-(4-氟苯基)甲基]哌嗪化合物的合成及生物活性

Synthesis and Bio-activity of 4-Substituted 1-[Bis(4-Fluoro-Phenyl)Methyl]Piperazine

目的 合成 4-取代的 1- [二 - ( 4-氟苯基 )甲基 ]哌嗪化合物 ,寻找优良的抗偏头痛药物。方法 以盐酸洛美利嗪为先导物 ,对其哌嗪 4位取代基进行修饰。结果和结论 合成了 11个未见文献报道的 4-取代的 1- [二 - ( 4-氟苯基 )甲基 ]哌嗪化合物。结构经 IR、1 HNMR、MS及元素分析确证。初步药理筛选结果显示 ,化合物 1 - 2 , 6 - 1 1 均有不同程度的钙拮抗活性 ,其中 2

AIM The purpose is to search for potent compounds with antimigraine. METHOD Lomerizine hydrochloride as a lead compound was modified in structure using different substituents at position 4 of piperazine. RESULTS and CONCLUSION Eleven 4-substituted 1-[bis(4-fluorophenyl)methyl]piperazine coupounds were designed and synthesized. These compounds were not reported previously and their structures were identified by IR, 1HNMR, MS and elemental analysis. The preliminary biological test showed that Ⅰ 1-2 and Ⅰ 6-11 have calcium antagonistic activity to different extent.