Liu Y. Synthesis of new agents for mycobacterioses based on 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids hydrazides

The paper deals with the search of new biologically active substances with the anti-mycobacterial action in the range of 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxy-lic acids hydrazides. The synthesis of acyl-, alkylidene- and pyridinylmethylenehydrazides of 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids, as well as 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbaldehydes, their thiosemicarbazones and 3-arylaminome-thylenequinoline-2,4-(1H,3H)-diones has been carried out and methods for their obtaining have been offered. The structure has been confirmed elementary analysis, spectroscopy NMR (including NOE, COSY, HMQC, HMBC methods), mass-spectrometry and X-ray structural analysis. The antimycobacterial properties of the substances synthesized have been studied. As a result, peculiarities of the "structure - biological action" relationship have been determined and 1-heptyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid pyridine-4-ylme-thylenehydrazide as a promising antimycobacterial agent can be recommended for further research.