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Synthesis and antiinflammatory activity of 2- (E) -benzylidene-5- (N-substituted aminomethyl) cyclopentanones

Dong, J.; Xu, L.; Qin, H.; Chen, S.; Ji, Z.; Wang, M.

Yao Xue Xue Bao 33(5): 344-349

1998

ISSN/ISBN: 0513-4870
PMID: 12017001
Document Number: 489288
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.

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