A new <i>N</i> -acylhydrazone oxadiazole derivative with activity against mycobacteria
<b>Aim:</b> To evaluate the anti<i>-Mycobacterium tuberculosis</i> (<i>Mtb</i>) potential of the hybrid oxadiazol-4-methoxynaphthalene (<b>6n</b>) derived from <i>N</i>-acylhydrazone (<b>4k</b>).<b>Materials & methods:</b> The study determined the minimal inhibitory concentration of (<b>6n)</b> against <i>Mtb</i> H<sub>37</sub>Rv and <i>Mtb</i> clinical isolates, potential combination of (<b>6n)</b> with anti-tuberculosis drugs and carried out time kill curve assay of <i>Mtb</i> H<sub>37</sub>Rv. Additional contribution for the analysis of <b>(6n)</b> was explored by <i>in silico</i> pharmacokinetics, and <i>in vitro</i> and <i>in vivo</i> cytotoxicity determinations.<b>Results:</b> The newly synthesized molecule (<b>6n)</b> demonstrated anti-<i>Mtb</i> activity, low cytotoxicity and selectivity for <i>Mtb.</i><b>Conclusion:</b> The derivative (<b>6n</b>) emerges as a potential anti-TB drug candidate.
Authors
- Rosilene Fressatti Cardoso (ORCID: https://orcid.org/0000-0001-6228-4780)
- Gisele F. Gauze (ORCID: https://orcid.org/0000-0002-1971-1983)
- Deisiany Gomes Ferreira (ORCID: https://orcid.org/0000-0001-6601-6046)
- Melyssa Negri (ORCID: https://orcid.org/0000-0003-2071-8872)
- Jonathan Rosa (ORCID: https://orcid.org/0000-0002-2407-6240)
- Regiane Bertin de Lima Scodro (ORCID: https://orcid.org/0000-0002-9129-2445)
- Izabella Ventura de Souza (ORCID: https://orcid.org/0000-0003-1083-6242)
- Andrew Matheus Frederico Rozada (ORCID: https://orcid.org/0000-0001-8151-7949)
- Katiany Rizzieri Caleffi-Ferracioli (ORCID: https://orcid.org/0000-0003-0345-1600)
- Eloísa Gibin Sampiron (ORCID: https://orcid.org/0000-0002-4337-0007)
- Maria Luiza Fróes da Motta Dacome (ORCID: https://orcid.org/0000-0001-5884-9902)
Institutions
- Universidade Estadual de Maringá (BR)
Publication Details
- Journal
- Future Microbiology
- Published
- 2024-10-23
- DOI
- https://doi.org/10.1080/17460913.2024.2412439
- Citations
- 1
- Primary Topic
- Mycobacterium research and diagnosis
- Type
- article
- Field-Weighted Citation Impact
- 0.39
Funders
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
- Conselho Nacional de Desenvolvimento Científico e Tecnológico