A new N -acylhydrazone oxadiazole derivative with activity against mycobacteria.

Autor: Souza IV; Postgraduate Program of Biosciences and Physiopathology, Department of Clinical Analysis and Biomedicine, State University of Maringa, Maringa, Parana, Brazil., Fróes da Motta Dacome ML; Postgraduate Program of Biosciences and Physiopathology, Department of Clinical Analysis and Biomedicine, State University of Maringa, Maringa, Parana, Brazil., Frederico Rozada AM; Department of Chemistry, State University Maringa, Maringa, Parana, Brazil., Rosa JS; Postgraduate Program of Biosciences and Physiopathology, Department of Clinical Analysis and Biomedicine, State University of Maringa, Maringa, Parana, Brazil., Sampiron EG; Postgraduate Program in Health Sciences, State University of Maringa, Maringa, Parana, Brazil., Ferreira DG; Postgraduate Program in Health Sciences, State University of Maringa, Maringa, Parana, Brazil., Gauze GF; Department of Chemistry, State University Maringa, Maringa, Parana, Brazil., Norman Negri MF; Postgraduate Program in Health Sciences, State University of Maringa, Maringa, Parana, Brazil., de Lima Scodro RB; Postgraduate Program in Health Sciences, State University of Maringa, Maringa, Parana, Brazil., Cardoso RF; Postgraduate Program of Biosciences and Physiopathology, Department of Clinical Analysis and Biomedicine, State University of Maringa, Maringa, Parana, Brazil.; Postgraduate Program in Health Sciences, State University of Maringa, Maringa, Parana, Brazil., Caleffi-Ferracioli KR; Postgraduate Program of Biosciences and Physiopathology, Department of Clinical Analysis and Biomedicine, State University of Maringa, Maringa, Parana, Brazil.
Jazyk: angličtina
Zdroj: Future microbiology [Future Microbiol] 2024 Oct 23, pp. 1-12. Date of Electronic Publication: 2024 Oct 23.
DOI: 10.1080/17460913.2024.2412439
Abstrakt: Aim: To evaluate the anti -Mycobacterium tuberculosis ( Mtb ) potential of the hybrid oxadiazol-4-methoxynaphthalene ( 6n ) derived from N -acylhydrazone ( 4k ). Materials & methods: The study determined the minimal inhibitory concentration of ( 6n) against Mtb H 37 Rv and Mtb clinical isolates, potential combination of ( 6n) with anti-tuberculosis drugs and carried out time kill curve assay of Mtb H 37 Rv. Additional contribution for the analysis of (6n) was explored by in silico pharmacokinetics, and in vitro and in vivo cytotoxicity determinations. Results: The newly synthesized molecule ( 6n) demonstrated anti- Mtb activity, low cytotoxicity and selectivity for Mtb. Conclusion: The derivative ( 6n ) emerges as a potential anti-TB drug candidate.
Databáze: MEDLINE