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 |
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Hauptverfasser: | , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
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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. |
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ISSN: | 1756-8919 1756-8927 |
DOI: | 10.4155/fmc-2018-0281 |