.2 - (e) - (4 - Methanesulfonyl-amino) Benzylidene Cyclopentanone Mannich Bases Synthesis And Antiinflammatory Activity Of Research

The development of NSAIDs and the correlation of COX-2 with inflammation were briefly introduced. On the basis of the structures of selective COX-2 inhibitors, a methanesulfonylamino group which was a anti-inflammatory active group was introduced into the Mannich base of substituted cyclopentanone possessing anti-inflammatory activity.In this thesis, thirteen new compounds, including eleven Mannich bases of 2-(E)-(4-methanesulfonylamino)benzylidenecyclopentanone were synthesized. The structures of thirteen compounds were identified by MS, 1H-NMR and IR spectra.The compounds were evaluated for anti-inflammatory activity. Preliminary pharmacological tests at a dose of 200mg/kg on xylene-induced mice ear edema, showed that two compounds, 2-(E)-(4-methanesulfonylamino)benzylidene-5-[N-(4-bromo)phenyl]aminomethylcyclopentanone and 2-(E)-(4-methane sulfonylamino)benzylidene-5-[N-(4-ethoxyl)phenyl]aminomethylcyclopen-tanone, exerted anti-inflammatory activity. Both of them showed inhibition of 21.7% and were as efficient as Indometacin at a dose of 10 mg/kg.