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Abstract

Aim: To study the effect of 5-R-thio-tetrazolo[1,5-с]quinazoline derivatives on the physical performance in different types of physical exercise. Materials and Methods: The experiments were performed on Wistar white male rats weighing 190-210 g. The investigated substances and a comparator, 2-ethylthiobenzymidazol hydrobromide, were injected intraperitoneally to animals OD during 5 days in ED 50 doses. Physical performance of rats was assessed by treadmill running tests at a speed of 42 m/min with a 10° slope angle and holding rats at a 15 rpm rotarod test. The study was performed on the day 5 of the experiment, 40 min after the past injection. Results and Discussion: We revealed that a 5-day course administration of 5-R-thio-tetrazolo[1,5-c]quinazoline derivatives at an ED 50 dose contributed to growing the length of a rat treadmill running. The results of the test presented that physical endurance of animals grew with compounds KB-10, KB-28, KB-51, and KB-55 by 47.1, 60.7, 32.3, and 46.0 %, respectively. The duration of holding rats on rotarods with a pharmacological correction was 41.2-71.4 % higher than in the control group. The dynamics of physical endurance against treadmill running and rotarod tests results in the group of animals administered the reference medicine, 2-ethylthiobenzymidazol hydrobromide, made up 50.7 and 59.4% compared to the control, respectively. Conclusion: KB-28 (sodium 2-(tetrazolo[1,5-c]quinazoline-5-iltio)acetate) demonstrated the greatest effect on physical endurance of study participants among all 5-R-thio-tetrazolo[1,5-c]quinazoline derivatives. This substance was not only similar with the reference medicine in efficacy but also had ED 50 19 times lower than reference actoprotector.

Biochemical aspects of KB-28 compound on physically loaded study subjects

“…The structural formula of KB-28 compound is as follows: In research, KB-28 was able to improve physical endurance of rat models under normal and augmented experimental loads. The above activity was manifested by an increase of the swimming length under normo-, hyper-and hypothermia settings [10,11]. The same manifestation was seen in rotated rod and treadmill run experiments [13,14].…”

“…Having analyzed the results obtained, we can draw a conclusion that influencing the biochemical processes in the study models is one of the mechanisms of the KB-28 actoprotective effect. [1,5-c]quinazoline-5-ylthio)acetate (KB-28 compound) was found to be a leader in the previous studies of actoprotective activity of new derivatives of 5-R-thio-tetrazolo [1,5-c]quinazoline under normal and augmented experimental conditions [10,11]. Derivatives of the above class of substances were synthesized by the staff of the Department of Organic and Bioorganic Chemistry of the Zaporizhzhia State Medical University [12].…”