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Structure-activity relationship of natural and synthetic coumarin derivatives against Mycobacterium tuberculosis

Authors:

Pires, Claudia T. A. [1] ; Scodro, Regiane B. L. [2] ; Cortez, Diogenes A. G. [3, 4] ; Brenzan, Mislaine A. [3] ; Siqueira, Vera L. D. [1] ; Caleffi-Ferracioli, Katiany R. [1] ; Vieira, Lucas C. C. [5] ; Monteiro, Julia L. [6] ; Correa, Arlene G. [4] ; Cardoso, Rosilene F. [1, 2]

 

Abstract:

Aim:Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated againstMycobacterium tuberculosisH(37)Rv reference strain and multidrug-resistant clinical isolates.Materials \& methods:Anti-M. tuberculosisactivity was evaluated by resazurin microtiter assay plate, and the cytotoxicity of natural and synthetic products using J774A.1 macrophages by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide.Results:Compounds1g,5,6,12and14were more active againstM. tuberculosisH(37)Rv and multidrug-resistant clinical isolates with minimum inhibitory concentration values ranging from 15.6 to 62.5 mu g/ml.Conclusion:These results demonstrate that the coumarin derivatives were active against multidrug-resistant clinical isolates, becoming potential candidates to be used in the treatment of resistant tuberculosis.

 

1   Programa de Pós-Graduação em Biociências e Fisiopatologia, Universidade Estadual de Maringá, 87020-900 Maringá, Paraná, 87020-900, Brazil

2   Programa de Pós-Graduação em Promoção da Saúde, Unicesumar – Centro Universitário, Maringá, Paraná, 87050-390, Brazil

3   Instituto de Engenharia, Universidade Federal de Mato Grosso, Cuiabá, Mato Grosso, 78060-900, Brazil

4   Laboratório de Síntese de Produtos Naturais – LSPN, Departamento de Química, Universidade Federal de São Carlos, São Carlos, São Paulo, 13565-905, Brazil

5   Programa de Pós-Graduação em Ciências da Saúde, Universidade Estadual de Maringá, Maringá, Paraná, 87020-900, Brazil

 

 

Link to article:    https://www.future-science.com/doi/10.4155/fmc-2018-0281