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.
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Title:Synthesis, Characterization and Anti-inflammatory Activity of N-(4- phenyl-1, 3-thiazol-2-yl)-N'-phenylureas
Volume: 13 Issue: 2
Author(s): Aneesa Fatima, Ravindra Kulkarni, Bhagavanraju Mantripagada, Asief Mohammed, Anusaya Birajdar and V.M. Chandrasheskar
Affiliation:
Keywords: Anti-inflammatory, 2-amino-4-phenyl thiazole, molecular docking, N-(4-phenyl-1, 3-thiazol-2-yl)-N'-phenyl urea, p38 kinase.
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.
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Fatima Aneesa, Kulkarni Ravindra, Mantripagada Bhagavanraju, Mohammed Asief, Birajdar Anusaya and Chandrasheskar V.M., Synthesis, Characterization and Anti-inflammatory Activity of N-(4- phenyl-1, 3-thiazol-2-yl)-N'-phenylureas, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2014; 13 (2) . https://dx.doi.org/10.2174/1871523013666140820154843
DOI https://dx.doi.org/10.2174/1871523013666140820154843 |
Print ISSN 1871-5230 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-614X |
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