3—甲基—4—甲氧羰基芬太尼类似物的合成与镇痛活性
Synthesis and Analgesic Activity of Analogs of 3-Methyl-4-Methoxycarbonyl Fentanyl
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摘要: 报道某些3-甲基-4-甲氧羰基芬太尼类似物的合成,顺反异构体的分离及其镇痛活性。实验结果表明,该类化合物具有与3-甲基芬太尼类和4-甲氧羰基芬太尼类相当的强效镇痛活性(活性最强的化合物18a镇痛强度为吗啡的2939倍),构效关系更类似于前者。顺式异构体的活性通常强于反式,且二者强度比较小,提示4-甲基羰基引入到3-甲基芬太尼类化合物分子中降低了3位甲基对阿片受体作用的选择性。Abstract: The synthesis, separation of diastereo-isomers and analgesic activities of some analogs of N-1-(2-phenylethyl)-3-methyl-4-methoxycarbonyl-4-piperidinyl-N-propionylaniline (3-methyl-4-methoxycarbonyl fentanyl) were reported. Preliminary pharmacological r