Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents

ISSN: 1875-614X (Online)
ISSN: 1871-5230 (Print)

Volume 15, 3 Issues, 2016

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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Inflammatory and Anti-Allergy Agents

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Claudiu T. Supuran
Neurofarba Department
University of Florence

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Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents

Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry, 13(3): 174-187.

Author(s): Saurabh Khadse, Vinod Ugale and Gokul Talele.

Affiliation: Department of Pharmaceutical Chemistry, R. C. Patel College of Pharmacy, Shirpur (Dhule), Maharashtra, India.


In an attempt to find a new class of anti-inflammatory agents, a series of novel benzamides 3 (ab1-ab16) was synthesized by utilizing some arylideneoxazolones 2(az1-az4) having 2-acetyloxyphenyl substitution on their second position. IR, 1H-NMR, 13C NMR and HRMS, confirmed the structures of these synthesized compounds. Among the tested benzamide compounds 3ab1, 3ab2, 3ab11 and 3ab16 showed promising anti-inflammatory activity with lessened propensity to cause gastro-intestinal hypermotility and ulceration when compared with standard Indomethacin. Virtual screening was performed by docking the designed compounds into the ATP binding site of COX-2 receptor to predict if these compounds have analogous binding mode to the COX-2 inhibitor.


Anti-inflammatory, benzamides, docking, gastro-intestinal hypermotility, ulcerogenic activity.

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Article Details

Volume: 13
Issue Number: 3
First Page: 174
Last Page: 187
Page Count: 14
DOI: 10.2174/1871523013666141017102257
Price: $58

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