(2014) Imidazo2,1-bthiazole derivatives as new inhibitors of 15-lipoxygenase. European Journal of Medicinal Chemistry. pp. 759-764.
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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, 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. © 2014 Elsevier Masson SAS.
| Item Type: | Article |
|---|---|
| Keywords: | arachidonate 15 lipoxygenase; hydrogen peroxide; imidazo2,1 bthiazole derivative; n (tert butyl) 3 phenyl 6 (p tolyl)imidazo2,1 bthiazol 5 amine; n (tert butyl) 6 (4 chlorophenyl) 3 phenylimidazo2,1 bthiazol 5 amine; n (tert butyl) 6 (4 methoxyphenyl) 3 phenylimidazo2,1 bthiazol 5 amine; n (tert butyl) 6 (4 nitrophenyl) 3 phenylimidazo2,1 bthiazol 5 amine; quercetin; unclassified drug, animal cell; Article; cell death; cell differentiation; cell viability; drug synthesis; hydrophobicity; IC50; molecular docking; nonhuman; oxidative stress; rat |
| Page Range: | pp. 759-764 |
| Journal or Publication Title: | European Journal of Medicinal Chemistry |
| Volume: | 87 |
| Publisher: | Elsevier Masson SAS |
| Depositing User: | ms soheila Bazm |
| URI: | http://eprints.ssu.ac.ir/id/eprint/8953 |
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