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Updated: Oct 3, 2025
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Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
3,5-dinitrobenzoylhydrazone derivatives as a scaffold for antituberculosis drug development
Tamires L Valverde1, Eloísa G Sampiron1, Débora C Montaholi1
1Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil.
Abstract:
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.
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