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    Protective effects of thiazolo[3,2-b]-1,2,4-triazoles on ethanol-induced oxidative stress in mouse brain and liver
    (Pharmaceutical Society Korea, 2005) Aktay, G; Tozkoparan, B; Ertan, M
    A series of 3-[1-(4-(2-methyIpropyl) phenyl) ethyl] - 1 2,4-triazole-5-th ion e (1) and its bicyclic condensed derivatives 6-benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones (IIa-IIf) were investigated for the prevention of ethanol-induced oxidative stress in liver and brain of mice. Administration of ethanol (0.1 mL/mice, p.o.) resulted in a drop of total thiol groups (T-SH) and non-protein thiol groups (NP-SH), and an increase in thiobarbituric acid reactive substances (TBARS) in both liver and brain tissue of mice (p < 0.001). Among the compounds investigated (at a dose of 200 mg/kg, p.o.), I and IId ameliorated the peroxidative injury in these tissues effectively. Compounds IIa, IIc and IIe improved the peroxidative tissue injury only in brain. These findings suggest that certain condensed thiazolo-triazole compounds may contribute to the control of ethanol-induced oxidative stress in an organ selective manner.
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    Synthesis of some new pyridylethylated benzoxa(thia)zolinones with analgesic activitiy
    (Tubitak Scientific & Technological Research Council Turkey, 2004) Gökhan, N; Aktay, G; Erdogan, H
    Eighteen new 3-[2-(2-/4-pyridyl)ethyl]benzoxlinone(benzothiazolinone) derivatives were synthesized by reacting 2-/4-vinylpyridine and appropriate benzoxazolinones and benzothiazolinones. The analgsic activities of these compounds were investigated by modified Koster and hot-plate tests. Test results revealed that most of the compounds at 100 mg/kg dose levels have higher analgestic activities than acetylisalicylic acid. Compounds with bromo substituents on the phenyl ring in the 6-position of the main ring seemed to show less activity than those with fluorinated ones. Compound 6b showed remarkably high activity in the hot-plate test, although it was inactive in the Koster test. However compound 3a had statistically significant high peripheral analgesic activity at all doses compared to other compounds, although it was inactive in the hot-plate test.