1. Aminocarbonyl arylvinylbenzamides as gastric sparing anti-inflammatory agents.
- Author
-
Khadse SC, Talele GS, and Agrawal SS
- Subjects
- Animals, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Anti-Inflammatory Agents, Non-Steroidal chemistry, Benzamides chemical synthesis, Benzamides chemistry, Carrageenan, Diclofenac chemistry, Diclofenac pharmacology, Dose-Response Relationship, Drug, Edema chemically induced, Rats, Structure-Activity Relationship, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Anti-Inflammatory Agents, Non-Steroidal toxicity, Benzamides pharmacology, Benzamides toxicity, Stomach drug effects, Stomach Ulcer chemically induced
- Abstract
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, (1)H- and (13)C-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 20âmg/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., (Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2011
- Full Text
- View/download PDF