Gencheva V. Biological activity of S-substituted 2-methyl-4-mercapto-8-methoxyquinoline

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0408U003061

Applicant for

Specialization

  • 02.00.10 - Біоорганічна хімія

20-06-2008

Specialized Academic Board

Д 26.220.01

V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine

Essay

S-substituted 2-methyl-4-mercapto-8-methoxyquinoline. Search of effective bioregulators of a wide action spectrum in series S-substituted 2-methyl-4-mercapto-8-methoxyquinoline and an establishment of dependence structure-biological effect. Chemical synthesis, biological and biochemical methods, element analysis, a thin-layer chromatography, IR-, PMR-, UV-spectroscopy, chromato-mass-spectrometry, computer forecasting. S-substituted derivatives of 2-methyl-4-mercapto-8-methoxyquinoline were synthesized and were considered as low-toxic and nontoxic compounds (LD50 is within 566-2000 mg/kg). Basing on the model of oxidative stress in vivo (brain cerebrum ischemia) it was demonstrated that the injection of their nontoxic sodium salts in dose 1/50 LD50 affects the value of free radical oxidation and carbohydrate metabolism, as well as protects antioxidative enzyme activities (superoxiddismutase, catalase, glutationperoxidase, and the amount of ?-tocopherol). Convenient method of synthesis of sodium salt of2-hydroxy-3-(8-methoxy-2-methylquinolin-4-ylthio)propionic acid has been developed and its pre-clinical research was conducted. Sphere of use - bioorganic chemistry, medicine.

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