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合成了具有强效镇痛活性的3-甲基芬太尼衍生物1-(4-甲基-3-戊烯基)-3-甲基-4-(N-丙酰苯胺基)哌啶(1)及其顺(±)反-(±)-和顺-(+)-、顺-(-)-异构体。小白鼠热板试验结果表明,其异构体的构效关系类似于3-甲基芬太尼,但1-乙基的β-苯基被 Me_2C=CH 基取代后降低了分子对阿片受体作用的立体选择性。
A 3-methylfentanyl derivative 1- (4-methyl-3-pentenyl) -3-methyl-4- (N- propionanilide) piperidine was synthesized with potent analgesic activity (1) and its cis (±) trans- (±) -cis- (+) -, cis- (-) - isomer. The results of the hot plate test in mice showed that the structure-activity relationship of the isomers was similar to that of 3-methyl fentanyl, but the substitution of 1-ethyl-β-phenyl group by Me_2C = The role of the three-dimensional selectivity.