The antioxidant properties of1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-onederivatives under conditions of artificial oxidative stress in vitro
Journal Title: Saudi Journal of Medical and Pharmaceutical Sciences - Year 2017, Vol 3, Issue 1
Abstract
Abstract: Experimental pharmacological researchof 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one derivatives.Determination of the nature of the effect of electron-donating and electron-withdrawing substituents in the phenyl fragment of the molecule on expression of the antioxidant activity.Analysis of some aspects of the "structure–activity" relationship.Derivatives of1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one were synthesized by Hantzsch method. Experimental pharmacological research was carried out on the model of artificial oxidative stress using the emulsion of egg-yolk lipoproteins in vitro as a substrate of oxidation. The substances of group 1 with methyl substituents and group 2 with chlorine substituent posseses pronounced antioxidantactivity. The substances of group 2 with methoxy substituentposseses moderate antioxidantactivity. Introduction of any substituents leads to a significant change in the level and direction of antioxidant activity of the substances; and it depends on the chemical nature and orientation of the substituents in the phenyl fragment of the molecule.Among the compounds under research four compounds can be recommended as potential antioxidants for further screening studies. Keywords: 1,3-thiazole derivatives, in vitro, artificial oxidative stress, antioxidant activity
Authors and Affiliations
Lina Perekhoda, Hanna Yeromina, Irina Drapak, Natalia Kobzar, Olexandr Smolskiy
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