Synthesis And Anti-Inflammatory And Analgesic Activities Of Pyrrolizinone Derivatives

This paper is about the study of synthesis and activities of a new type of nonsteroidal anti-inflammatory drugs (NSAIDs), 3H-1,2-dihydro-1-pyrrolizinone.Based on the SAR summarized, seventeen new compounds of 3H-1,2-dihydro-1-pyrrolizinone were designed and synthesized. Their chemical structures were confirmed by IR, ¹H-NMR, ¹³C-NMR and MS.The anti-inflammatory and analgesic activities were tested on xylene-induced mouse ear edema and acetic acid-induced mouse writhing. The preliminary pharmacological studies showed that most of the compounds had significant anti-inflammatory and/or analgesic activities. Among them, the analgesic activity of W-11, W-13, W-14, W-15, W-17 were comparable to ibuprofen. W-11 had better anti-inflammatory activity.Some new SAR of these compounds was discussed.