3,5-dinitrobenzoylhydrazone derivatives as a scaffold for antituberculosis drug development.

Background: The development of drugs is essential to eradicate tuberculosis. Materials & methods: Sixteen 3,5-dinitrobenzoylhydrazone ( 2-17 ) derivatives and their synthetic precursors 3,5-dinitrobenzoylhydrazide ( 1 ) and methyl ester ( 18 ) were screened for their anti- Mycobacterium tuberculosis ( Mtb ) potential. Results: Twelve compounds had minimum inhibitory concentration (MIC) ranging from 0.24 to 7.8 μg/ml against the Mtb strain. The activity was maintained in multidrug-resistant Mtb clinical isolates. Only compound ( 17 ) showed activity against nontuberculous mycobacteria. The compounds exhibited a limited spectrum of activity, with an MIC >500 μg/ml against Gram-positive and -negative bacteria. Compounds ( 2 ), ( 5 ) and ( 11 ) showed a synergistic effect with rifampicin. An excellent selectivity index value was found, with values reaching 583.33. Conclusion: 3,5-dinitrobenzoylhydrazone derivatives could be considered as a scaffold for the development of antituberculosis drugs.