EXPERIMENTAL RESEARCH OF DIURETIC PROPERTIES OF NEW 7-METHYL-N-BENZYL-8- SUBSTITUTED THEOPHYLLINE

Autor: O. P. Matviychuk, O. M. Hladchenko, A. V. Matviychuk, D. H. Ivanchenko
Jazyk: angličtina
Rok vydání: 2016
Předmět:
Zdroj: Фармацевтичний часопис, Vol 0, Iss 2 (2016)
ISSN: 2414-9926
2312-0967
Popis: EXPERIMENTAL RESEARCH DIURETIC PROPERTIES OF NEW 7-METHYL-N-BENZYL-8-SUBSTITUTED THEOPHYLLINE. Matviychuk O.P., Gladchenko O.M., Matviychuk A.V., Ivanchenko D.G. National University of Pharmacy Zaporozhye State Medical University Introduction. Diuretics are widely used in the treatment of a number of diseases caused by a variety of diseases, in which the need to use these drugs. In many cases there is a clinical need to increase urine output for excretion of fluid, reducing its content in tissues and serous cavities. Especially great role of diuretic drugs in the treatment of patients with chronic congestive heart failure. Thanks to properties diuretics cause increased excretion of sodium and water from the body is given a real opportunity to actively influence the fluid and electrolyte disturbances in these patients. The use of diuretic agents (hydrochlorothiazide, furosemide, etacrynic acid, etc.) are often accompanied by side effects, which primarily relate to fluid and electrolyte homeostasis, acid-base balance, carbohydrate metabolism, phosphate, creatinine and uric acid. The search for new medicines that improve the functional activity of the kidneys, is one of the urgent problems of modern experimental pharmacology. Synthesis of modified analogs of biologically active substances of natural origin is a priority for research to address this issue. Given this, it was interesting to conduct forecasting of possible types of pharmacological activity of derivatives 7,8-disubstituted theophylline using the «PASS» (Predectum of Activity Spectra for Substances: Complex & Training), whose work is based on an analysis of dependencies "structure - activity". The results of the computer forecast derivative 7-p-metylbenzyl-8-substituted theophylline showed a high likelihood of these types of compounds of pharmacological activity, diuretical, spasmolytical, psycho-stimulant, analgesic, anti-inflammatory. Investigation methods. To solve the tasks as object of study was first taken 20 compounds synthesized derivatives of 7-n-metylbenzyl-8-substituted theophylline. The influence of new derivatives of p-20 metylbenzyl-8-substituted theophylline on renal function was performed on white male rats weighing 140-190 g Ye.B.Berhina method [1; 5]. Animals in the experiment were in individual metabolic cages adapted to collect urine. Number of animals in the group amounted to 5. Investigated derivatives intragastric administered at a dose of 1/100 of LD50. After 30 minutes, the rats were injected with tap water at the rate of 3 ml per100 g body weight. Urine recorded 2 hours to 4 hours. As a comparison drug used hydrochlorothiazide (hypothiazid) production «Sanofi Aventis»,France. Results and discussion. Study diuretic activity 7-p-metylbenzyl-8-substituted theophylline showed that these compounds affect renal function. Most of the studied derivatives showed diuretic activity, which used to range from 23.2% to 153.7%. Marked diuretic effect compound found 14 - 7 p-metylbenzyl-8-p-bromobenzylidenhidrazynoteofilin which stimulates excretory renal function in rats and increases urine 4 hours of observation at 153.7% (p
Databáze: OpenAIRE
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