Targeted Hybridization: Pyrazine‐2‐Carbohydrazide Derivatives as Promising Antitubercular and Antimicrobial Leads

Abstract In an attempt to identify a new pharmacological lead which should be more potent than the established drug pyrazinamide, a molecular hybridization technique was applied to fuse two pharmacophore moieties: pyrazine‐2‐carbohydrazide ( 1 ) and diphenyl ether/piperazinyl derivative ( 2 ), to isolate a new series of hybrid molecules. The synthesized compounds were tested in vitro for their antibacterial and antimycobacterial properties against E. coli and S. aureus and Mycobacterium TB H 37 Rv strains. In comparison to the reference medication (pyrazinamide) these compounds exhibited moderate antitubercular and antibacterial action, with a MIC value of 15.625–125 µg/mL. All the synthesized molecules were characterized through IR, NMR and mass spectrometry. Docking studies were carried out in order to have better understanding related to protein and ligand receptor interactions.