Pyrrolidine Hydrochloride And Quinoline Derivatives Synthesis And Analgesic Activity Study

The syntheses and structure-activity relationships (SAR) for 6,6a, 7,11b-tetrahydro-5H-p-yrrolizino[2,1-c]quinoline derivatives were studied in this thesis.It has been found in our laboratory that the derivatives of pyrrolizinone manifested anti-inflammatory and analgesic activities. In order to search for the potential agents having better activities and lower toxicities, we designed some new derivatives of pyrrolizinone on the basis of previous studies.6,6a, 7, 11b-Tetrahydro-5H-pyrrolizino[2,1-c]quinoline showed excellent analgesic activity in the derivatives of pyrrolizinone. Based upon the structures of opioid analgesics, the analogues of 6, 6a, 7,11b-tetrahydro-5H-pyrrolizino[2,1-c]quinoline were designed and synthesized via Mannich reaction, amine exchange reaction, reduction reaction, cyclozation r-eaction, alkylation/ acylation reaction using pyrrolizinone as the starting material.Most of the compounds synthesized here showed analgesic activities in vivo. Among of them, RZY-5, RZY-18 demonstrated significant analgesic activities.Some SAR of these compounds were summarized.