Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Author(s): Aneesa Fatima, Ravindra Kulkarni, Bhagavanraju Mantripagada, Asief Mohammed, Anusaya Birajdar and V.M. Chandrasheskar

DOI: 10.2174/1871523013666140820154843

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Synthesis, Characterization and Anti-inflammatory Activity of N-(4- phenyl-1, 3-thiazol-2-yl)-N'-phenylureas

Page: [112 - 120] Pages: 9

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Abstract

A series of N-(4-phenyl-1, 3-thiazol-2-yl)-N'- phenylureas (5a-z) was synthesized from 2-amino-4-substituted phenylthiazoles and phenylisocyanates. The newly synthesized compounds were characterized by IR, 1H NMR and Mass spectral data. All the twenty six N-(4-phenyl-1, 3-thiazol-2-yl)-N'-phenylurea derivatives were screened for antiinflammatory activity by following carrageenan induced rat paw edema method. Among the compounds screened, N-[4- (4-methoxy phenyl)-1, 3-thiazol-2-yl)-N'-phenylurea and N-[4-(4-methoxy phenyl-1, 3-thiazol-2-yl)-N'-(4-bromophenyl) urea were found to be more potent. The molecular docking interaction of aforementioned urea compounds revealed the traditional type II p38 kinase inhibitor’s interactions in the DFG out active site.

Keywords: Anti-inflammatory, 2-amino-4-phenyl thiazole, molecular docking, N-(4-phenyl-1, 3-thiazol-2-yl)-N'-phenyl urea, p38 kinase.

Graphical Abstract