Nikitin V. Synthesis, physico-chemical and biological properties of 2-R-4(3H)quinazolone(thione) derivatives

Object - 2-R-4(3Н)quinazolone and 2-R-4(3Н)quinazolinthione derivatives; methods - synthesis, NMR-, IR-, mas-, chromato-mass-spectroscopies, TLC, quantum-chemical calculations, pharmacological screening, regression analysis; novelty - the preparative methods of synthesis were developed and series of new 2-(R-phenyletenyl-2)-, 2-[4-(R1-phenyl)-3-R-butadien-1,3-yl-1]- and other 2-R-4(3H)-quinazolones, 2-(R-phenyl-etenyl-2)-quinazolin-(3Н)-4-thiones, 2-(2-R-quinazoli-ne-4-ylthio)-1-R1-ethane(propane-1)-ones, a(b)- (2-R-quinazoline-4-ylthio)-carbo-xylic acids and their functional derivatives were obtained, pharmacological screening of antiradical, antioxidant, hepatoprotective, antiamnestic, antifungal, antimicrobial, anticancer activity and ability to have action upon oxidative protein modification has been carried out, a group of highly active substances was identified, the values of descriptor series for investigated compounds were calculated and with a help of regression analysis correlating equationswere determined; the outcomes - are introduced into scientific and educational process of pharmaceutical chemistry, organic chemistry departments of National Pharmaceutical University, pharmaceutical, organic and bioorganic chemistry department of L'viv National Medical University; area - pharmacy.