Repository of Research and Investigative Information

Repository of Research and Investigative Information

Shahid Sadoughi University of Medical Sciences

Imidazo 2,1-<i>b</i> thiazole derivatives as new inhibitors of 15-lipoxygenase

(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
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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