Diuretic activity of some 4- and 3-thio-substituted 1,2,4-triazoles with fluorophenyl fragments

Abstract

Diuretics increase the volume of urine and sodium excretion, and therefore are often used to remove excess fluid from the body during various diseases, including hypertension, heart and kidney failure, nephrotic syndrome, cirrhosis, etc. Until now, a wide range of diuretics is known, but none of them is completely safe and has a number of side effects. The aim of the work is to investigate the diuretic activity of 1,2,4-triazole derivatives containing fluorophenyl substituents at the fifth position of the 1,2,4-triazole fragment, as well as to establish the relationship between “chemical structure and diuretic action” among derivatives 1,2,4-triazole. Materials and methods. To study the effect on kidney function, six groups of animals with seven rats each were used. When studying water diuresis, rats were kept on a constant diet with free access to water. Before water loading (5 % of body weight), rats were fasted for 2 hours without food and water. Since all tested compounds were insoluble in water, they were administered orally as an aqueous suspension stabilized with Tween-80. The compounds were administered at a dose of 1/10 LD50. Results. The diuretic activity of 28 new compounds of a number of substituted 1,2,4-triazole-3-thiols, which according to their chemical structure belong to different classes of compounds, was investigated. Conclusions. Analysis of the results of diuretic activity indicates that there are a number of compounds whose activity is higher than hypothiazide, as well as a compound that exceeds the activity of furosemide.

Keywords

• diuretic effect
• 1 2 4-triazole derivatives
• “structure – action”