Korniyenko V. Pharmacological activity of 7,8-di-, 1,7,8-trisubstituted of xanthine and ammonium salts of 3,7-di- and 1,3,7-trimethylimidazo[1,2-f]xanthines-8-acetic and propionic acids.

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0410U002582

Applicant for

Specialization

  • 14.03.05 - Фармакологія

04-06-2010

Specialized Academic Board

Д 64.605.01

National University of Pharmacy

Essay

On the basis of results of the computer prognosis the research of pharmacological activity of the firstly synthesized 7,8-di- and 1,7,8-trisubstituted of 3-methylxanthine (comp.1-17), ammonium salts of 1,7-disubstituted of 3-methylxanthinyl-8-thioacetic acid (comp.18-29), ammonium salts of 3,7-di- and 1,3,7-trimethylimidazo[1,2-f]xanthinyl-8-acetic acid (comp. 30-46) and ammonium salts of 3,7-di- and 1,3,7-trimethylimidazo[1,2-f]xanthinyl-8 propionic acid (comp. 47-60) has been carried out. Exciting on CNS activity monoethanolaminic salt of 3,7-dimethylimidazo[1,2-f]xanthinyl-8 propionic acid (comp. 15) has shown. Deprimic action compound 10 - 1-p-methylbenzyl-7-methyl-8-benzoylmethylthio-3-methylxanthine has shown, which increases the threshold of aggressiveness on 37,3%. Antihypoxic action has been found out in compound 57, which increases duration of rats in the closed space on 46% . Analgesic activity has shown by compound 50 -N-benzyl-N-hydroxyethylaminic salt of 3,7-dimethylimidazo[1,2-f]xanthinyl-8 propionic acid, which decreases quantity of acetic convulsions on 47,9%. Compound 44 -morpholinic salt of 1,3,7-trimethylimidazo[1,2-f]xanthinyl-8 propionic acid has shown anti-inflammatory activity, oppressing of development of flogogenic edema of paw for rats on 45,6%. Compound 42 - piperidinic salt of 1,3,7-trimethylimidazo[1,2-f]xanthinyl-8 acetic acid (condi-tional name pimidoxane) increases urea excretion on 128,2% and and exceeds the action of hy-potiazide in 1,95 times. Pimidoxane has the expressed sodiumuretic and diuretic effect due to diminishing of reabsorbtion of sodium ions in tubuli renalis of nephrons of kidneys, improve-ment of filter function in the vascular glomerulis of kidneys, activating of the kallikrein-kinin system and synthesis of prostaglandins of PGE2, low toxicity does not have ulcerogenic action on the mucous of stomach and duodenum.

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