Synthesis and antituberculosis activity of N-R-amides 1-hydroxy-3-oxo-6,7 dihydro-3H, 5H-pyrido [3,2,1-ij] quinoline-2-carbonic acids

Abstract

A series of 1-hydroxy-3-oxo-6,7-dihydro-3H, 5H-pyrido [3,2,1-ij]quinoline-2-carboxylic acid heterylamides was synthesized in high yields and purity. The chemical structure of the synthesized compounds was confirmed by 1H NMR spectra and elemental analysis. Analysis of the antimycobacterial properties subjected to microbiological screening shows that compound 3a and 3c with pyridine and 4-ethoxycarbonylmethylthiazole fragments showed 100% activity in relation to the used strain. A complete loss of activity was observed in derivatives 5a-c with a 4- methoxyanilide hydrochloride fragment and a 4-R-piperazine nucleus.