[Synthesis and antiinflammatory activity of 2-(E)-benzylidene-5-(N-substituted aminomethyl) cyclopentanones].
Nineteen kinds of 2-(E)-benzylidene-5-(N-substituted aminomethyl) cyclopentanones were synthesized via Mannich reaction or amine exchange reaction and identified spectrometrically. One compound exhibited significant antiinflammatory activity, showing obvious inhibitory effect on xylene-induced mice ear swelling, carrageenin-induced rats paw edema and increased capillary permeability induced with acetic acid in mice. Its ED50 values in these inflammatory models were calculated to be 67.8 mg.kg-1, 25.3 mg.kg-1 and 41.8 mg.kg-1 respectively, nearly equal to those of ibuprofen and aspirin.
Dong
J
J
Shenyang Pharmaceutical University, Shenyang 110015.
Xu
L
L
Qin
H
H
Chen
S
S
Ji
Z
Z
Wang
M
M
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D002199:Capillary Permeability / Q000187:drug effects; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000494:pharmacology; D004487:Edema / Q000188:drug therapy; D005260:Female; D008297:Male; D051379:Mice; D015394:Molecular Structure; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003517:Cyclopentanes; C007201:cyclopentanone