Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents

Three new series of 4-hydroxy-8-trifluoromethyl-quinoline derivatives were synthesized through multi step reactions. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 5j was evidenced by X-ray crystallographic study. The newly synthesized title compounds were evaluated for their antimicrobial activities including antimycobacterial activity. Amongst the tested compounds, 5b, 5e, 5h, 5j, 6c and 7c displayed promising antimicrobial activity. The mode of action of these active compounds was carried out by docking of receptor enoyl-ACP reductase with newly synthesized candidate ligands, 5b, 5e, 5h, 5j and 6c. Three new series of 4-hydroxy-8-trifluoromethyl-quinoline derivatives were synthesized and the most effective compounds have a MIC value of 0.625μg/mL against Mycobacterium tuberculosis H37Rv. [Display omitted] ▸New series of quinoline carbohydrazone derivatives were synthesized. ▸X-ray crystallographic study of the title compound 5j was carried out. ▸In vitro antibacterial and antimycobacterial screening were carried out. ▸Compounds 5b, 5e, 5h, 5j and 6c showed substantial antitubercular activity. ▸Docking studies were carried out.