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Aminocarbonyl Arylvinylbenzamides as Gastric Sparing Anti‐inflammatory Agents
Author(s) -
Khadse Saurabh C.,
Talele Gokul S.,
Agrawal Surendra S.
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000096
Subject(s) - benzamide , chemistry , carrageenan , anti inflammatory , amide , edema , diclofenac , nucleophile , biological activity , pharmacology , stereochemistry , biochemistry , in vitro , medicine , catalysis
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 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.