Oleksiyenko T. Synthesis, physicochemical and biological properties of 2-R-4-methyl-6-R'-sulfonylqinolines.

This thesis is devoted to the directed search for new biologically active substances among derivatives of 2-substituted 4-methylquinolines. As a result, the optimal ways of synthesis of 4-methyl-2-chloroquinoline-6-alkyl(heteryl-, aryl-)sulfonamides, which served as the basis for obtaining 2-alkyl(heteryl-, aryl-)amino-4-methylquinoline-6-sulfonamides and some 2-alkoxy-4-methylquinoline sulfo¬derivatives have been developed. The comparative analysis of obtaining methods of 2-amino-4-methylquinoline sulfoderivatives has been conducted first. It has been shown that the most convenient synthesis of 2-alkoxy-4-methylquinoline-6-benzensulfones and 2-alkoxy-4-methylquinoline-6-phenylsulfamides is carried out by nucleophilic substitution of corresponding 4-methyl-2-chloroquinolines, which were obtained by previous substitution of carbonyl group of 4-methyl-1,2-dihydroquinoline-2-ones. Antimicrobial, diuretic, haemostatic and anticoagulant activity of new compounds has been studied, some structure-activity relationships have been revealed. As a result, diethylamide of 2,7-dichloro-4-methylquinoline-6-sulfonic acid, which has significant diuretic activity, has been recommended for further biological researches.