Paper
[Synthesis and antiinflammatory activity of 2-(E)-benzylidene-5-(N-substituted aminomethyl) cyclopentanones].
Published May 1, 1998 · J. Dong, L. Xu, H. Qin
Yao xue xue bao = Acta pharmaceutica Sinica
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Abstract
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.
The synthesized 2-(E)-benzylidene-5-(N-substituted aminomethyl) cyclopentanone shows significant antiinflammatory activity, with ED50 values comparable to those of ibuprofen and aspirin.
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