А.A. Safonov, N. V. Rachok, T. A. Samura, Ye.G. Knysh

ACTOPROTECTIVE ACTIVITY OF NEW DERIVATIVES OF 4-AMINO-5-(THIOPHENE-2-YLMETHYL)-4H-1,2,4-TRIAZOLE-3-THIOL

Scientific supervisor - O. I. Panasenko

Keywords: derivatives of 1,2,4-triazole, actoprotective activity.

Introduction: the Search for completely new biologically active compounds involves the synthesis of substances, studying their physico-chemical properties and proof of structure and the study of pharmacological and biological activities. Interest to scientists is the core of 1,2,4-triazole. After analyzing the literature, it should be noted that depending on the substituents on the 1,2,4-triazole ring of the synthesized compounds may be actoprotective, antimicrobial, antifungal, analgesic, antiviral, hepatoprotective and other activities [1-4].

The high pace of modern people life necessarily leads to lower and sometimes to depletion of physical and mental abilities of the body. For people, especially those who live in larger cities acquired great importance chronic fatigue syndrome, which is haracterized by the reduction of protective mechanisms of adaptation, immunity and health. The main reason for this are the long-term physical and psychological load average and high intensity. The solution to this problem is the use of modern drugs actoprotector.

The aim of our work was to study act-protective activity of new derivatives of 4-amino-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiol.

Methods and materials: the Study was conduct on a group of white nonlinear rats by weight: 200-260 g. On the study of act-protective activity, we used a method of forced swimming (Bobkov, Y. G., 1984) with a load of 10% of the weight of the rat. The load recorded at the base of the tail of animals. Swimming was perform until exhaustion, which was fix after a 10-second immersion of laboratory animals under the water. Rats were immers alone in a container large value of water layer exceeding 60 cm water Temperature was 30-350C. The studied compounds as well as the standard of comparison – riboxinum injected intraperitoneally 20 minutes prior to the start of the dive animals at a dose of 100 mg/kg. The swim was count in seconds. For comparison, a control group of animals treated with intraperitoneal saline for 20 minutes before immersion.

Results and discussion: we Investigated 10 act-protective effect of new compounds derivatives of 4-amino-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiol. It is establish that the synthesized substances have a moderate act-protective effect. 2 compound exceeds activity of the standard riboxinum.

Conclusions: As a result of research was identified 2 compounds that exceeded comparison standard riboxinum. So, in this way, the introduction of the thiophene-2-ylmethylene radical in the molecule 1,2,4-triazole produces the increase in act-protective action of the derivatives of 1,2,4-triazole.

Literature:

1. Beat I. M., Mikhaylyuk Is. A. study of the hepatoprotective activity of derivatives 1, 2, 4-triazole //Pharmaceutical journal. – 2011. – №. 6. – S. 61.

2. Bushueva, I. V., etc. the Use of morpholine 2-[5-(pyridin-4-yl)-1, 2, 4-triazole-3-LTO] acetate for the treatment and prevention of certain diseases. – 2014.

3. Parchenko V. Antiviral activity of derivatives of 1, 2, 4-triazole //Pharmaceutical journal. – 2011. – №. 3. – S. 49-53.

4. Bily, A. K., etc. Antimicrobial and antifungal activity of {2-[3-hetaryl-1H-1, 2, 4-triazole-5-yl] phenyl} amine and their products heterocyclic.