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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 的活性与阳性对照药盐酸洛美利嗪接近
Aim To synthesize 4-substituted 1- [di- (4-fluorophenyl) methyl] piperazine compounds and to find excellent antimigraine drugs. Methods Lomerizine hydrochloride as a leader, its 4-piperazine substituents were modified. RESULTS AND CONCLUSIONS Eleven novel 4-substituted 1- [di- (4-fluorophenyl) methyl] piperazine compounds were synthesized. The structure was confirmed by IR, 1 HNMR, MS and elemental analysis. Preliminary pharmacological screening results showed that compounds 1 - 2 and 6 - 1 1 all had different degrees of calcium antagonistic activity, of which the activity of 2 was close to that of positive control Lomerizine hydrochloride