Brazhkо O. The biological activity of the derivatives of 2-methyl(phenyl)substituted (quinoline-4-ylthio)carboxylic acids

The derivatives of 2-methyl(phenyl)substituted (quinoline-4-ylthio)carboxylic acids. The search for effective bioregulators-neuroprotective agents among the 2-methyl(phenyl) substituted (quinoline-4-ylthio)carboxylic acids. Virtual screening (PASS-prognosis), QSAR-analysis, chemical synthesis, biological and biochemical methods (study of toxic action, antimicrobial activity, analgesic, diuretic effect, antioxidant activity (AOA) in vitro, state antioxidant (AO) cell protection system neurocytes of rats ), physico-chemical methods (elemental analysis, thin layer chromatography, NMR-spectroscopy, chromato-mass spectrometry). The least toxicity relative species investigated derivatives exhibit alkoxy(methoxy)groups, their introduction into the benzene ring quinoline resulted in a significant decrease (in 5-20 times) acute toxicity of 4-thioquinoline is shown. The presence of antiradical activity of the synthesized compounds was defined. The compounds with analgesic, antimicrobial, antiradical, antioxidant, diuretic action were discovered among derivatives of 2-methyl(phenyl) substituted (quinoline-4-ylthio) carboxylic acids and their structural analogues. The structure of the leader was founded - the disodium salt of 2-(2-methyl-5,8-dimethoxyquinoline-4-ylthio)succinate acid, is a relatively harmless (VI class of toxicity) neurometabolic antioxidant-cerebroprotector with a complex mechanism of action