5,6-diaryl-2,3-dihydro-1-pyrrolizinone derivatives synthesis and antiiflammatory and analgesic activities
Zhao, L.Q.; Yang, Z.; Zhang, S.F.
Yao Xue Xue Bao 36(4): 258-261
2001
ISSN/ISBN: 0513-4870 PMID: 12580052 Document Number: 527127
To search for more potent and less toxic antiinflammatory and analgesic activity compounds. A series of 5,6-diaryl-2,3-dihydro-1-pyrrolizinone derivatives were designed and synthesized based on the structures of diarylheterocyclic COX-2 selective inhibitors. Their structures were determined on the basis of spectal data (IR, MS and 1HNMR). Their antiinflammatory and analgesic activities in vivo were tested by xylene-induced mouse ear edema model and acetic acid-induced mouse writhing model p.o. dose of 200 mg.kg-1. Seventeen new compounds (1-17) were synthesized. Many of these compounds showed antiinflammatory and analgesic activities. Compound 3, 8, 11, 14 and 15 showed antiinflammatory activities more potent than ibuprofen. Compound 9, 10 and 11 showed analgesic activities comparable to ibuprofen. These compounds are regarded to be promising to develop new potent drugs.