Kravtsova V. The search of new local anaesthetics in the range of amide derivatives of oxoquinoline-3-carboxylic acids

The paper deals with the search of new biologically active substances with the local anaesthetic action in the range of 2-oxo-1,2-dihydroquinoline-3-carboxylic acids dialkylaminoalkylamides. The synthesis of N-R-amides of 2-oxo-quinoline-3-carboxylic acids, of their hydrogenated analogs, as well as 1-R-3-(2-dialkyl-aminoethyl)-1Н-quinazoline-2,4-diones has been carried out and methods for their obtaining have been offered. The structure was confirmed by ultimate analysis, spectroscopy NMR (including NOE, COSY, HMQC, HMBC methods), mass-spectrometry, chromatomass-spectrometry and X-ray structural analysis. The local anaesthetic properties of the substances synthesized have been studied. As a result, peculiarities of the "structure - biological action" relationship have been determined and hydrochloride of 2-diethylaminoethylamide of 1-і-butyl-2-оxо-1,2-dihydro-quinoline-3-carboxylic acid as a promising local anaesthetic agent can be recommended for further research.