Davydenko O. Synthesis, physical, chemical properties and biological activity of substituted 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids and their derivatives

The paper deals with the search of new biologically active substances in the range of 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids and their functional derivatives, such as esters, N-R-amides and 4-amino analogues. The preparatory methods for their obtaining have been offered and the synthesis of the compounds mentioned has been carried out. Their structure has been confirmed by elemental analysis, NMR 1Н spectra, and in some cases by counter synthesis and X-ray diffraction analysis. The ability of the substances synthesized to block opioid receptors, as well as their analgesic properties have been studied. It allows to reveal the "structure - biological action" relationships and recommend 1-allyl-4-hydroxy-6,7-dimethoxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid (3-mor-pholin-4-ylpropyl)-amide hydrochloride as a perspective opioid receptors antagonist of a new chemical class for further research.