Kryskiw O. Synthesis 4-oxo-3,4-dihydroquinazolines from amides and hydrazides of 2-N-acylanthranillic acid, their chemical and biological properties

Interaction of anthranilohydroxamic acid, its sodium salt and amide of an-thranilic acid with derivatives of carboxylic acids was explored. It was determinate and direction of the reaction depends of a substituent near the nitrogen atom of amidgroup of anthranilamides. At presence of substituents which show the increased electrophylic properties (OH-group), acetylation and cyclodehydratacion with formation -R-3-hydroxy-4-oxo-3,4-dihydroquinazolines take place consistently. In other case acylic derivatives appear, their cyclization under various conditions leads to formation of cyclic imides or 2-R-4-oxo-3,4-dihydroquinazolines. On the base of synthesized 4-oxo-3,4-dihydroquinazolines the new condensed tricyclic systems was obtained. The convent method of synthesis of 2-R-3-hydroxy[1,2,4]triazino[6,1-b]quinazolin-4,10-diones on the basis of izatoic anhydride, carboxylic acids hy-drazides, etoxalilchloride and hydroxylamine without separation of intermediate products was proposed.Virtual screening (program PASS) of the synthesized compounds was carried out, taking into account its results; microbiological and pharmacological researches were carried out. By the data microbiological researches it was determined, that de-rivatives of 4-oxo-3,4-dihydroquinazoline and heterocyclic compounds on their basis show the high rate of antimicrobic activity. The project of ASD for N-hydroxyamid-3-atcetylamino-4-oxo-3,4-dihydroqunazolin-2-carboxyllic acid, which show the highest rate of antimicrobic activity and low toxicity was developed. It was deter-mined, that researched compounds show the low rate of diuretic and antinflammatory activityand low toxicity was developed.