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.
Graphical Abstract
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Title:Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents
Volume: 13 Issue: 3
Author(s): Saurabh Khadse, Vinod Ugale and Gokul Talele
Affiliation:
Keywords: Anti-inflammatory, benzamides, docking, gastro-intestinal hypermotility, ulcerogenic activity.
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.
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Khadse Saurabh, Ugale Vinod and Talele Gokul, Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2014; 13 (3) . https://dx.doi.org/10.2174/1871523013666141017102257
DOI https://dx.doi.org/10.2174/1871523013666141017102257 |
Print ISSN 1871-5230 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-614X |
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