Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 87, Issue -, Pages 759-764Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.10.011
Keywords
Imidazo[2,1-b]thiazole; Enzyme inhibitors; 15-Lipoxygenase; Docking study
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Funding
- Research Council of Tehran University of Medical Sciences
- Iran National Science Foundation (INSF)
- Drug Design and Development Research Center, Tehran University of Medicinal Sciences
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A series of 3,6-diphenylimidazo[2,1-b]thiazol-5-amine derivatives was synthesized and evaluated as potential inhibitors of 15-lipoxygenase. Among the synthesized compounds, 51 bearing 2,4,4-trimethylpentan-2-yl pendent group was the most active compound, being two times more potent than reference drug quercetin. Also, the docking study revealed that 5i interacts properly with target enzyme 15-LOX and hydrophobic interactions have important role in the binding process. Besides, the protective effect of 5i against oxidative stress-induced cell death in differentiated PC12 cells was evaluated. The results showed that compound 5i significantly protected PC12 cells against H2O2-induced cell death at concentrations less than 10 mu M. (c) 2014 Elsevier Masson SAS. All rights reserved.
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