Iorio M A, Casy A F
J Med Chem. 1978 Aug;21(8):812-5. doi: 10.1021/jm00206a019.
A number of N-substituted 2,3-dimethyl-3-arylpiperidines having an m- or p-arylhydroxyl were prepared and evaluated for analgesic agonist and antagonist properties. The diastereomeric N-allyl and N-cyclopropylmethyl derivatives behaved as pure potent antagoinists. Substitution of the arylhydroxyl from the meta to the para position resulted in a net fall of the antagoinist activity.
制备了一系列具有间位或对位芳基羟基的N-取代2,3-二甲基-3-芳基哌啶，并对其镇痛激动剂和拮抗剂特性进行了评估。非对映异构体N-烯丙基和N-环丙基甲基衍生物表现为纯强效拮抗剂。芳基羟基从间位取代变为对位取代导致拮抗剂活性净下降。
