Hydrazone, benzohydrazones and isoniazid-acylhydrazones as potential antituberculosis agents.

Autor:	Sampiron EG; Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Costacurta GF; Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Baldin VP; Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Almeida AL; Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Ieque AL; Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Santos NC; Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Alves-Olher VG; Department of Chemistry, Federal Institute of Paraná, Paranavaí, Paraná, 87703-536, Brazil., Vandresen F; Department of Chemistry, Federal Technological University of Paraná, Londrina, Paraná, 86057-970, Brazil., Gimenes AC; Department of Chemistry, Federal Institute of Paraná, Paranavaí, Paraná, 87703-536, Brazil., Siqueira VL; Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Caleffi-Ferracioli KR; Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Cardoso RF; Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil.; Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil., Scodro RB; Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil.
Jazyk:	angličtina
Zdroj:	Future microbiology [Future Microbiol] 2019 Jul; Vol. 14, pp. 981-994. Date of Electronic Publication: 2019 Aug 06.
DOI:	10.2217/fmb-2019-0040
Abstrakt:	Aim: To evaluate the potential of three benzohydrazones ( 1 - 3 ), four acylhydrazones derived from isoniazid (INH-acylhydrazones) ( 4 - 7 ) and one hydrazone ( 8 ) as antituberculosis agents.  Materials & methods: Inhibitory and bactericidal activities were determined for the reference Mycobacterium tuberculosis ( Mtb ) strain and clinical isolates. Cytotoxicity, drug combinations and ethidium bromide accumulation assays were also performed. Results: The tested compounds ( 1 - 8 ) presented excellent antituberculosis activity with surprisingly inhibitory (0.12-250 μg/ml) and bactericidal values, even against multidrug-resistant Mtb clinical isolates. Compounds showed high selectivity index, with values reaching 1833.33, and a limited spectrum of activity. Some of the compounds ( 2 & 8 ) are also great inhibitors of bacillus efflux pumps. Conclusion: Benzohydrazones and INH-acylhydrazones may be considered scaffolds for the development of new anti- Mtb drugs.
Databáze:	MEDLINE
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