Synthesis And Analgesic Activity Of The Tetrahydro Quinoline Compounds

The study on synthesis and structure-activity relationships (SAR) of 4-(1H-pyrrol-2-yl)-tetrahydroquinoline derivatives is reported in this paper.Tetrahydropyrrolizino[2, 1-c]quinoline derivatives were discovered to be a lead compound with highly analgesic activities. Based on the SAR of tetrahydropyrrolizino[2, 1-c]quinoline derivatives and Oripavine analgesic agents, twenty new compounds of 4-(1H-pyrrol-2-yl)-tetrahydroquinoline derivatives were designed and synthesized. Their chemical structures were characterized by ~1H-NMR and MS.Acid-induced mice writhing was used to evaluate the analgesic activity. Pharmacological studies showed that most of the synthesized compounds displayed notable analgesic activities at a dose of 200 mg/kg. The activities of compounds FLY-1, FLY-6, FLY-12, FLY-14, FLY-15 are comparable to that of morphine at a dose of 10 mg/kg. They could be regarded as valuable compounds for further study. Some new SAR of these compounds was summarized.