[5,6-diaryl-2,3-dihydro-1-pyrrolizinone derivatives synthesis and antiiflammatory and analgesic activities].
OBJECTIVE
To search for more potent and less toxic antiinflammatory and analgesic activity compounds.


METHODS
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.


RESULTS
Seventeen new compounds (1-17) were synthesized. Many of these compounds showed antiinflammatory and analgesic activities.


CONCLUSIONS
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.
Zhao
L Q
LQ
Shenyang Pharmaceutical University, Shenyang 110015, China.
Yang
Z
Z
Zhang
S F
SF
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D004487:Edema / Q000188:drug therapy; D051379:Mice; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011758:Pyrroles