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

Author:

Valverde Tamires L1ORCID,Sampiron Eloísa G1ORCID,Montaholi Débora C1ORCID,Baldin Vanessa P2ORCID,Insaurralde Diego DR3ORCID,Alves-Olher Vanessa G4ORCID,Siqueira Vera LD2ORCID,Caleffi-Ferracioli Katiany R2ORCID,Cardoso Rosilene F12ORCID,Vandresen Fábio3ORCID,Scodro Regiane BL1ORCID

Affiliation:

1. Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil

2. Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil

3. Department of Chemistry, Federal Technological University of Paraná, Londrina, Paraná, 86036-370, Brazil

4. Department of Chemistry, Federal Institute of Paraná, Paranavaí, Paraná, 87703-536, 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.

Publisher

Future Medicine Ltd

Subject

Microbiology (medical),Microbiology

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