The study of the diuretic activity of new benzyl acid derivatives

Authors

DOI:

https://doi.org/10.24959/cphj.20.1534

Keywords:

benzyl acid derivatives, diuretic activity, Berkhin method, hypothiazide

Abstract

Diuretics increase the urine volume and sodium excretion, and therefore, they are often used to remove the excess fluid from the body during various diseases, including hypertension, heart and kidney failure, nephrotic syndrome, cirrhosis, and a number of other diseases.

Aim. To study the diuretic activity of new benzyl acid derivatives.

Materials and methods. The diuretic activity of the test compounds and the reference drugs – hypothiazide and furosemide was studied in intact white rats weighing 200.0 ±20.0 g by the method of Ye. B. Berkhin. Benzyl acid derivatives in the doses of 12 mg/kg and the reference drugs – hypothiazide and furosemide in the doses of 50 mg/kg and 20 mg/kg, respectively, were administered orally as aqueous solutions 60 min before the start of the experiment. A spontaneous diuretic activity was assessed by the amount of urine excreted in 2, 4 and 6 hours after the start of the experiment.

Results. In the course of the study it was found that the diuretic activity was shown by substances KMS-68, KMS-70 and KMS-229 in 2 hours from the beginning of the experiment. The most active was KMS-229 (5-oxo-6,6-diphenyl-5,6-dihydro-4-H-benzo[d]thieno[3,4-b]azepine-3-carboxylic acid methyl ester), which significantly increased the volume of urine excreted compared to the control and the activity of hypothiazide by 2 times.

Conclusions. The study of the diuretic activity of new derivatives of benzyl acid has been conducted. Compounds KMS-229 and KMS-70 have been shown to act as short-acting diuretics.

Author Biographies

N. M. Tryschuk, National University of Pharmacy

Candidate of Medicine (Ph.D.), associate professor of the Department of Pharmacotherapy

I. V. Kireyev, National University of Pharmacy

Doctor of Medicine (Dr. habil.), professor, head of the Department of Pharmacotherapy

K. M. Sytnik, National University of Pharmacy

Candidate of Pharmacy (Ph.D.), associate professor of the Organic Chemistry Department


S. V. Kolisnyk, National University of Pharmacy

Doctor of Pharmacy (Dr. habil.), professor of the Department of Analytical Chemistry

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Published

2020-09-03

Issue

Vol. 24 No. 3 (2020)

Section

Pre-clinical studies of new drugs

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