Future microbiology · 2019
Hydrazone, benzohydrazones and isoniazid-acylhydrazones as potential antituberculosis agents.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод пока не подготовлен
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Sampiron Eloísa G, Costacurta Giovana F, Baldin Vanessa P, Almeida Aryadne L, Ieque Andressa L, Santos Nathally Cs, Alves-Olher Vanessa G, Vandresen Fábio, Gimenes Ana Cr, Siqueira Vera Ld, Caleffi-Ferracioli Katiany R, Cardoso Rosilene F, Scodro Regiane Bl
Аннотация
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.