取代哌啶基苯骈咪唑啉酮类衍生物的合成及镇痛作用

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。

SYNTHESIS AND ANALGESIC ACTIVITY OF A SERIES OF SUBSTITUTED PIPERIDYL BENZIMIDAZOLINONE

Substituted piperidyl benzimidazolinone derivatives exert a wide range of pharmacological effects according to different substituents in position-1 of piperidine ring. These include tranquillizing, antihypertensive and analgesic activities and so on. The syntheses and analgesic activities of a series of substituted piperidyl benzimidazolinone derivatives as potential analgesics are reported in this paper. In mouse hot plate test most of these compounds showed analgesic activity and 1-{1-[1-(ptolyl)-ethyl]-4-piperidyl}-3-(2-cyanoethyl)-2-benzimidazolinone(I_h) was found to be the most potent, with a potency more than 500 times that of morphine. Introduction of a methyl group in position-3 of the piperidine ring markedly decreased the analgesic activity.