Protective effect of thiazolo[5,4-b]indole in toxic pulmonary edema

Abstract

Antiedematous activity of new thiazolo[5,4-b]indole derivatives containing a fragment of isothiourea and characterized by higher antihypoxic activity compared to known antihypoxants was studied on a model of toxic edema of the lungs in mice. Compounds exhibiting high activity on two models of hypoxia (hypobaric and hemic) better protected from lung edema than compounds active only in hypobaric hypoxia.

Acid‐catalyzed One Pot Synthesis of Thiazolo[4,5‐b]indolamines from α‐Diazoimidamides and Thioureas

“…The indole and thiazole rings in various natural and synthetic products have generated interest of many research teams because of their useful biological properties. Different structural types of thiazoloindoles are identified as cyclin‐dependent kinase II inhibitor to prevent/reduce the severity of epithelial cell toxicity [7] . Several structural types of thiazoloindoles can be distinguished with regard to the position of the fusion between thiazole, benzene, and pyrrole rings.…”

“…Different structural types of thiazoloindoles are identified as cyclin-dependent kinase II inhibitor to prevent/reduce the severity of epithelial cell toxicity. [7] Several structural types of thiazoloindoles can be distinguished with regard to the position of the fusion between thiazole, benzene, and pyrrole rings. Among them, five selected types of thiazoloindoles, i. e. thiazolo[3,2-a]-, [8] -[3,4-a]-, [9] - [5,4-b]-, [10] -[5,4-e]-, [11] and -[4,5e]indoles [12] have been reported.…”

“…Several cruciferous plants secrete thiazinoindoles [14,15] A,B (Figure 1) which are produced as defense chemicals in response to fungal attack. Thiazolo [5,4-b]indole C shows good pharmaceutical properties, [7] for example, as anti-edematous, and anti-hypoxic activities. However, thiazolo [4,5-b]indole D is known as 5HT 4 receptor antagonists in humans.…”

Modeling vibrational spectra of indole in water

“…The biological activity of natural indole compounds stimulates unwavering interest in them owing to the creation of therapeutic drugs based on them [1][2][3][4]. One of the principal reasons for such attention to indole is the high specificity of natural compounds that facilitates significantly transport processes through cell membranes.…”

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

“…The antihypoxic effects of these compounds were demonstrated on the models of hypobaric, hypercapnic, and hemic hypoxia, their activities being comparable or even superior to those of amtisole (reference drug) [1]. Thiasolo [5,4-b]indole derivatives exhibited membranotropic activity [9], antiedematous [3] and hepatoprotective effects [2], indicating their high biological activity directed to many targets. It is also known that other antihypoxants of similar condensed indole structures containing fragments of isothiourea also exhibited actoprotective activity [4,7].…”