El Kayal W. Synthesis, physicochemical and pharmacological properties of aryl-(alkyl)amides of (2,4-dioxo-/2-thio-4-oxo)-quinazolin-3-yl)acetic acids

The dissertation provides a practical solution to the scientific problem of a targeted search for potential anticonvulsants among quinazolin-4(3H)-one derivatives. According to the experimental studies results, the structure modification of quinazolin-4(3H)-one was substantiated, approaches to the synthesis of 2-(2,4-dioxo-/2-thioxo-4-oxo)-1,4-dihydroquinazolin-3(2H)-yl)acetic acid were developed as a building block of the study were developed, a targeted synthesis of their alkyl/arylacetamide derivatives was carried out, their physicochemical properties were determined, and their structure was proved. A potential innovative API - 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)-N-[(2,4-dichlorophenyl)-methyl]-acetamide having a wide spectrum of anticonvulsant action on chemotoxic and electroshock convulsion models, low toxicity, and a lack of muscle relaxant action, was found in result of realization of a complex of step-by-step in silico and in vivo studies of its pharmacological properties. Besides, multifactorial implementation of the anticonvulsant effect of the mentioned compound has also been proven