本文报道取代哌啶基苯骈咪唑啉酮类衍生物的合成及镇痛活性。这类衍生物一般都具有吗啡样的镇痛作用(小鼠,ip,热板法),其中化合物1-{1-[1-(对甲苯基)乙基]-4-哌啶基}-3-(2-氰乙基)-2-苯骈咪唑啉酮(I_h)的镇痛强度为吗啡的500多倍。哌啶环的3位引入甲基后,镇痛作用明显下降。 This paper reports the synthesis and analgesic activity of substituted piperidinylbenzimidazolone derivatives. Such derivatives generally have a morphine-like analgesic effect (mouse, ip, hot plate method) in which the compound 1- {1- [1- (p-tolyl) ethyl] The analgesic strength of 3- (2-cyanoethyl) -2-benzimidazolone (I_h) was more than 500 times that of morphine. After the methyl group of piperidine ring was introduced into the methyl group, the analgesic effect was obviously decreased.