Abstract
A series of new Coumarin hydrazone oxime scaffolds were synthesised as potential anti-TB agents.The structures of the scaffolds were confirmed by spectroscopic and analytical techniques.X-ray crystallography confirmed the structure of compound 6-methyl-4-((((Z)-((E)-3-(2-phenylhydrazono)butan-2-ylidene)amino)oxy)methyl)-2H-chromen-2-one(5a).The coumarin hydrazone oxime scaffolds were tested in-vitro against the Mycobacterium tuberculosis H_(37)Rv strain,and Vero cells were used to assess cytotoxicity.Compound 5b was obtained as the hit candidate,exhibiting MIC 0.78 μg/mL,showing more potent anti-TB activity than Rifamycin and comparable activity to Isoniazid.There was minimal cytotoxicity observed against Vero cells for the most active compounds,indicating a good safety-profile.In addition,the most diligent compound 5b demonstrated substantial binding interactions at the PDB:4DQU enzyme’s active site and also displayed greater C-score value than that of 4DQU ligand which validates the observed results.
NSTL