201989-28-8Relevant academic research and scientific papers
Aminocarbonyl arylvinylbenzamides as gastric sparing anti-inflammatory agents
Khadse, Saurabh C.,Talele, Gokul S.,Agrawal, Surendra S.
, p. 292 - 300 (2011/11/05)
Some (E/Z)-aminocarbonyl arylvinylbenzamides (B1-B15) were synthesized, evaluated for anti-inflammatory activity and ulcerogenic tendency, and their effect on gastro-intestinal motility in the rats was studied. These benzamides comprising of aliphatic unsaturated region situated between two amide linkages were synthesized by nucleophilic ring opening of appropriate azlactones (AZ1-AZ4) by suitable amines. The characterization of newly synthesized benzamides was performed by IR, 1H- and 13C-NMR, mass and elemental analysis. Amongst the tested compounds, benzamide B1, B2, B4, B5, and B13 were able to produce comparable or superior anti-inflammatory activity at 10 and 20 mg/kg p.o. dose with respect to standard diclofenac in carrageenan induced rat paw edema model with lessened propensity to cause gastro-intestinal hypermotility and were found to have nil tendencies to generate gastric ulcers. A series of N-[(E/Z)-2-(4-substituted/unsubstitutedphenyl)-1-{[arylamino] carbonyl} vinyl]benzamides (B1-B15) was synthesized by utilizing easily accessible starting material 4-substituted/unsubstituted benzylidene-2- phenyloxazol-5-one (AZ1-AZ4) and subjected to anti-inflammatory activity, gastrointestinal motility, and gastric damage studies in rats. Copyright
