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

In the thesis, the mechanism and the development of the NSAIDs were introduced. We designed a series of compounds, with the ideal : a methanesulfonyl group which was an anti-inflammatory active group was introduced into the Mannich base of substituted cyclopentanone. I started the synthesis work with 4-methanesulfonyl benzaldehyde and cyclopentanone, and got 13 new compounds ,including eleven Mannich bases derivatives of 2-(E)-(4-methanesulfonyl)denzylidene cyclopentanone. All the structures of the compounds were identified by ~1H-NMR and MS.All the compounds were evaluated for anti-inflammatory activity. Preliminary pharmacological tests showed that 2-(E)-(4-methanesulfonyl) benzylidene-5-[N-(4-methoxyl)phenyl]aminomethyl cyclopentanone(M-3), 2-(E)-(4-methanesulfonyl)benzylidene-5-[N-(4-methoxyl)phenyl]aminomethyl cyclopentanone(M-4), and 2-(E)-(4-methanesulfonyl) benzylidene-5-(N-dimethy)aminomethyl cyclopentanone hydrochloride(M-11) exerted good anti-inflammatory activity on xylene-induced ear edema in mice at the dose of 200mg/kg, superior to that of Indomethacin at the dose of 10mg/kg. The inhabitation rate of the 3 compounds was showed in the range of 47-50%.