| Autor: |
Tamires L Valverde, Eloísa G Sampiron, Débora C Montaholi, Vanessa P Baldin, Diego DR Insaurralde, Vanessa G Alves-Olher, Vera LD Siqueira, Katiany R Caleffi-Ferracioli, Rosilene F Cardoso, Fábio Vandresen, Regiane BL Scodro |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Future microbiology. 17 |
| ISSN: |
1746-0921 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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