(2014) Imidazo 2,1-<i>b</i> thiazole derivatives as new inhibitors of 15-lipoxygenase. European Journal of Medicinal Chemistry. pp. 759-764. ISSN 0223-5234
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Abstract
A series of 3,6-diphenylimidazo2,1-bthiazol-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.
Item Type: | Article |
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Keywords: | Imidazo2,1-bthiazole Enzyme inhibitors 15-Lipoxygenase Docking study possible involvement 5-lipoxygenase lipoxygenase expression potent Pharmacology & Pharmacy |
Page Range: | pp. 759-764 |
Journal or Publication Title: | European Journal of Medicinal Chemistry |
Journal Index: | WoS |
Volume: | 87 |
Identification Number: | https://doi.org/10.1016/j.ejmech.2014.10.011 |
ISSN: | 0223-5234 |
Depositing User: | Mr mahdi sharifi |
URI: | http://eprints.ssu.ac.ir/id/eprint/30213 |
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