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

Eight coumarin derivatives ( ) obtained from natural (-)-mammea A/BB ( ) and 13 synthetic coumarins ( ) had their cytotoxicity and biological activity evaluated against H Rv reference strain and multidrug-resistant clinical isolates. Anti- activity was evaluated by resazurin microtiter assay plate,...

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Veröffentlicht in:Future medicinal chemistry 2020-09, Vol.12 (17), p.1533-1546
Hauptverfasser: Pires, Claudia Ta, Scodro, Regiane Bl, Cortez, Diógenes Ag, Brenzan, Mislaine A, Siqueira, Vera Ld, Caleffi-Ferracioli, Katiany R, Vieira, Lucas Cc, Monteiro, Júlia L, Corrêa, Arlene G, Cardoso, Rosilene F
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Sprache:eng
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Zusammenfassung:Eight coumarin derivatives ( ) obtained from natural (-)-mammea A/BB ( ) and 13 synthetic coumarins ( ) had their cytotoxicity and biological activity evaluated against H Rv reference strain and multidrug-resistant clinical isolates. Anti- activity 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. Compounds , , , and were more active against H Rv and multidrug-resistant clinical isolates with MIC values ranging from 15.6 to 62.5 μg/ml. 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.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2018-0281