A.A. Safonov, Knysh Ye.G

Zaporozhye State Medical University

Department of Toxicologycal and Inorganic Chemistry

DIURETIC ACTIVITY OF 4-(R-IDENEAMINO)-5-(THIOPHEN-2-YLMETHYL)-4H-1,2,4-TRIAZOLE-3-THIOLS

Scientific adviser: Panasenko AI

Arterial hypertension - a condition in which blood pressure is greater than 140 mm Hg. Art. (as a result of at least three measurements made at different times on the background of a calm environment, we must not take the medication as raising and lowering pressure).

Hypertension affects 20-30% of the adult population. Up to 50 years of age the disease is more common in men after 50 years - for women.

One effective method of treatment of this disease is the use of diuretic drugs.

Modern pharmaceutical market has a huge variety of products in this area. But most of them require improvement by reducing toxicity and increasing efficiency. The task of the modern national pharmacy is to create a new original drug, which could compete with foreign both in price and in the activity. Prospective napryamki in danomu planі Yea synthesis novih Spoluka, yakі mіstyat kernel 1,2,4-trіazolu [2, 3]. Sered pohіdnih danogo number znaydenі preparations posaconazole, іtrakonazol, trazodone, alprazolam, kombіstim, avesstim.

The aim of our work was to study the diuretic activity of 4-(R-ideneamino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiols.

Materials and methods research. To study the effects on renal function has been used 6 groups of animals to 7 rats each. In the study of water diuresis in rats maintained on a constant diet with free access to water. To water stress (5% of body weight) rats were kept for 2 hours without food and water. Water-soluble compounds surveyed intraperytonalno injected with the rules of asepsis and antisepsis, water-insoluble - orally in the form of an aqueous suspension stabilized Tween-80. The compounds administered at a dose of 1/10 LD50. Urine was measured every hour for 4 hours. Urine that allocated control group of animals (which received no experimental compounds) received 100% [1].

Research and analysis of the experimental data was performed in comparison with the reference diuretic furosemide.

The research results are processed by modern statistical methods of analysis on a personal computer using, including the standard software package Microsoft Office 2010 (Microsoft Excel) and «STATISTICA® for Windows 6.0». Calculated arithmetic mean (M) and standard error of the mean (± m). The reliability of inter-group differences in experimental data set using Student t-test. We used 3 levels of statistical significance of differences of research results - p <0.05; P <0.01; and p <0.001 [4].

To study the diuretic activity were selected among the compounds 10 4- (R-ideneamino) -5- (thiophen-2-ylmethyl) -4H-1,2,4-triazole-3-thiols. The statistical data processing was found that the two compounds are close to the action of furosemide.

Conclusions

1. It has been studied the diuretic activity of newly synthesized 4- (R-ideneamino) -5- (thiophen-2-ylmethyl) -4H-1,2,4-triazole-3-thiols by Berchin EB

2. To study the diuretic activity were selected 10 compounds in a number of 4- (R-ideneamino) -5- (thiophen-2-ylmethyl) -4H-1,2,4-triazole-3-thiols 2 of which are close to the action of furosemide .

References:

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2. Вивчення впливу на функцію нирок S-похідних 5-(фуран-2-іл)-4-R₁-1,2,4-тріазол-3-тіонів / В.В. Парченко, О.І. Панасенко, Є.Г. Книш, Б.П. Зоря // Запорож. мед. журн. -2007.- №6. – С. 117-119.

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