Synthesis and antimycobacterial activity of N′-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives

The present article describes a series of twenty-six N′-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide (4–29), which were synthesized and evaluated for their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette–Guerin (BCG). Afterwards, the non-cytotoxic compounds (4, 6, 8, 15, 21, 23, 24, 27 and 28) were assessed against Mycobacterium tuberculosis ATCC 27294 using the micro plate Alamar Blue assay (MABA) and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. The compounds 6, 23, 27 and 28 exhibited a significant activity (50–100 μg/mL) when compared with first line drugs such as pyrazinamide and were not cytotoxic in their respective MIC values.

Graphical abstractA series of twenty-six pyrazine derivatives have been synthesized and evaluated against M. tuberculosis. Compounds 6, 23, 27 and 28 exhibited a significant activity (50–100 μg/mL).Figure optionsDownload full-size imageDownload as PowerPoint slide