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

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

Journal Name: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Volume 13 , Issue 3 , 2014

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Abstract:

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.

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

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Article Details

VOLUME: 13
ISSUE: 3
Year: 2014
Page: [174 - 187]
Pages: 14
DOI: 10.2174/1871523013666141017102257
Price: $58

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