Investigation of actoprotective activity in a range of 6-N-R-tetrazolo[1,5-c]quinazolin-5(6H)-ones

Antypenko, O. M.; Коваленко, С. И.; Trzhetsinsky, S. D.

doi:10.14739/2310-1210.2016.1.64023

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“…The promising ones in this respect are derivatives of quinazoline. [7][8][9][10] According to the results of previous studies, among 15 new 5-R-thio-tetrazolo[1,5-c]quinazoline derivatives we chose four compounds that most increased duration of swimming test under conditions of normo-, hyper-and hypo-thermia. [11][12][13] The above substances were synthesized at the department of organic chemistry of Zaporizkyi State Medical University under the leadership of professor Antypenko et al [8] To find a leading compound, it was reasonably to investigate the effect of the most active compounds on the physical endurance of rats.…”

Section: Original Articlementioning

confidence: 99%

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Kryvoviaz

2017

AJP

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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.

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Section: Original Articlementioning

confidence: 99%

Untitled

Kryvoviaz

2017

AJP

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Investigation of actoprotective activity in a range of 6-N-R-tetrazolo[1,5-c]quinazolin-5(6H)-ones

Cited by 1 publication

References 2 publications

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