Antihypoxants, Thiasolo[5,4-b]Indole Derivatives, Increase Exercise Performance in Rats and Mice

Abstract

The actoptrotective activity of 12 new antihypoxants of the thiasolo[5,4-b]indole series was studied on the model of treadmill running until exhaustion 1 and 24 h after intraperitoneal injection. Highly active compounds more effective than the reference drugs bemithyl and phenamine were found. They increased exercise performance 1 or 24 h after injection or maintained high performance throughout 24 h.

Department of Pharmacology of the Military Medical Academy in the 21st century: New achievements based on historical traditions (2000–2023)

“…В исследовании П.А. Торкунова [32,33,39,40] скрининговой моделью для оценки токсического отека легких и изучения эффективности лекарственных средств при поражении пульмонотоксикантами был выбран отек легких, вызванный фосгеном, у мелких лабораторных грызунов (мыши). Модель позволила оценить выраженность отека легких по легочному коэффициенту, а также эффективность профилактики и лечения токсического отека легких на ранней стадии и на стадии разрешения патологического процесса.…”

“…Его применение позволило предотвратить как формирование токсического отека легких, так и смертность отравленных животных. Из числа изученных новых производных тиазолоиндола наиболее выраженным профилактическим действием обладали соединения бромтиазоло [4,5-b]индола гидробромид и бромтиазоло [4,5-b]индол, лечебным действием -бромтиазоло [4,5-b]индола сукцинимид [39,40].…”

Hypoxia and antihypoxants, focus on brain injury

“…Effective antioxidants include ethomersol (5-ethoxy-2-ethylthiobenzimidazole), synthesized in the Department of Pharmacology of the Military Medical Academy; the biochemical and physiological effects of this agent are mediated by activation of protein synthesis and enzymes involved in energy metabolism and antioxidant systems [14]. The metabolic type of action of ethomersol is responsible for its significant protective properties in cerebrovascular disturbances of hypoxic origins [4]. The fact that ethomersol has actoprotective properties of nonexhausting nature leads us to expect its use to produce effective restoration of functional and metabolic lesions of the brain in the post-traumatic period.…”

“…To avoid overuse of medications for combined treatment of patients with CCT, it is necessary to synthesize new preparations with specific pharmacological activity. Antihypoxant bemithyl (2-ethylthio-benzimidazole hydrobromide) possesses nootropic and mild psychostimulant activity and fully conforms these requirements [4,8,9]. Here we studied the cerebroprotective effect of individual and combined treatment with the antihypoxant bemithyl and antidepressant pyrazidol in animals with CCT characterized by different resistance to hypoxia.…”

Synthesis, Antimicrobial Activity and Molecular Docking of Some Novel 2-Aryl-4H-[1,3]-thiazolo[4,5-b]indoles

“…The significance of thiazolo indoles in medicinal chemistry arises from their reported activities in various therapeutic areas, including antimicrobial, anti-inflammatory and anticancer properties [6][7][8]. Additionally, the ability of these compounds to interact with specific biological targets has sparked interest in exploring their potential as lead compounds for drug development [9][10][11][12][13]. In an urgent quest for novel and effective drugs, especially in the context of tuberculosis and bacterial infections in SARS-CoV-2 (COVID- 19), the investigation of thiazolo-indoles emerges as a promising avenue for discovering potent antitubercular agents [14].…”