The synthesis and anti-inflammatory and analgesic activities of Mannich bases, pyrrolo[1,2-a] pyrazine-1-one derivatives were reported in this paper.In the research of pyrrolizinones of nonsteroidal anti-inflammatory drugs (NSAIDs), it has been proved that pyrazinones showed remarkable anti-inflammatory and analgesic activities. Based on the reported pyrazinones in our laboratory, seventeen new Mannich bases of pyrazinone have been designed and synthesized, which structures have been confirmed by IR, ~1H NMR and MS.The results of pharmacological tests show that most of the compounds have notable anti-inflammatory and/or analgesic activities at a dose of 200mg/kg. The compounds LJ-10, LJ-11 and LJ-12 have valuable anti-inflammatory activities. Some SAR of these compounds is found from the studies above. |