Hydrazone, benzohydrazones and isoniazid-acylhydrazones as potential antituberculosis agents

Future Microbiology
Eloísa G SampironRegiane Bl Scodro

Abstract

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.

References

Jun 16, 2001·Antimicrobial Agents and Chemotherapy·I Orme, UNKNOWN Tuberculosis Drug Screening Program
Jul 18, 2002·Antimicrobial Agents and Chemotherapy·Juan-Carlos PalominoFrançoise Portaels
Mar 17, 2004·Toxicon : Official Journal of the International Society on Toxinology·R Manjunatha Kini
May 26, 2004·Bioorganic & Medicinal Chemistry·Gildásio A SilvaCarlos A M Fraga
Nov 19, 2004·Drug Metabolism and Pharmacokinetics·Fumiyoshi Yamashita, Mitsuru Hashida
Nov 1, 2006·European Journal of Medicinal Chemistry·K K Vijaya RajB K Sarojini
Oct 13, 2007·Journal of Chemical Information and Modeling·Tingjun HouYouyong Li
Oct 26, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sevim Rollas, S Güniz Küçükgüzel
Mar 4, 2008·The Journal of Antimicrobial Chemotherapy·Liliana RodriguesLeonard Amaral
Dec 10, 2008·Acta Tropica·Rodrigo Hinojosa ValdezCelso Vataru Nakamura
Nov 19, 2010·Jornal brasileiro de pneumologia : publicaça̋o oficial da Sociedade Brasileira de Pneumologia e Tisilogia·Marcos Abdo ArbexFernando Augusto Fiúza de Mello
Jan 29, 2011·Nature·Anil KoulKoen Andries
Mar 12, 2011·The Journal of Antimicrobial Chemotherapy·Paula Aline Zanetti CampanerutRosilene Fressatti Cardoso
Jan 28, 2012·European Journal of Medicinal Chemistry·Abraham GarcíaGildardo Rivera
Oct 3, 2013·Tuberculosis·Katiany R Caleffi-FerracioliRosilene F Cardoso
Mar 29, 2014·Memórias do Instituto Oswaldo Cruz·Claudia Terencio Agostinho PiresRosilene Fressatti Cardoso
Dec 1, 2004·Drug Discovery Today. Technologies·Christopher A Lipinski
Sep 13, 2014·Expert Opinion on Therapeutic Patents·Rodolfo do Couto MaiaCarlos Alberto Manssour Fraga
Feb 17, 2015·Journal of Microbiological Methods·Aline Lemes CastilhoRosilene Fressatti Cardoso
Mar 18, 2015·Methods in Molecular Biology·Julie Early, Torey Alling
Jun 28, 2015·Experimental Parasitology·Izabel Galhardo DemarchiMaria Valdrinez Campana Lonardoni
Apr 12, 2016·Tuberculosis and Respiratory Diseases·Yon Ju RyuCharles L Daley
Jan 17, 2017·Drug Discovery Today·Liliana RodriguesJosé A Ainsa
Oct 11, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Carlos R PolaquiniLuis O Regasini

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Citations

Apr 30, 2021·Microbial Drug Resistance : MDR : Mechanisms, Epidemiology, and Disease·Eloísa Gibin SampironRegiane Bertin de Lima Scodro
May 31, 2021·Trends in Microbiology·Mark LawsKhondaker Miraz Rahman

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