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  • Title: Imidazo[2,1-b]thiazole derivatives as new inhibitors of 15-lipoxygenase.
    Author: Tehrani MB, Emami S, Asadi M, Saeedi M, Mirzahekmati M, Ebrahimi SM, Mahdavi M, Nadri H, Moradi A, Moghadam FH, Farzipour S, Vosooghi M, Foroumadi A, Shafiee A.
    Journal: Eur J Med Chem; 2014 Nov 24; 87():759-64. PubMed ID: 25310714.
    Abstract:
    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, 5i 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 μM.
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