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

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.

Cite this article as:

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