Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents

A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis.

Graphical abstractSynthesis of a new series of quinoline-3-carbohydrazones is presented together with the pharmacological profiles. Compounds 13e, 13i, 13k, 14a, 14c, and 14i emerged as the lead molecules with MIC ranging 0.625–5 μg/mL and did not show toxicity on Vero cells up to 62.5 μg/mL which are in comparable with the present first line anti tuberculosis drugs.Figure optionsDownload full-size imageDownload as PowerPoint slide