Structure-activity relationship of natural and synthetic coumarin derivatives against Mycobacterium tuberculosis.
Future Med Chem
; 12(17): 1533-1546, 2020 09.
Article
en En
| MEDLINE
| ID: mdl-32820960
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 against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials &methods:
Anti-M. tuberculosis 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.Results:
Compounds 1g, 5, 6, 12 and 14 were more active against M. tuberculosis H37Rv and multidrug-resistant clinical isolates with MIC values ranging from 15.6 to 62.5 µg/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.Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Productos Biológicos
/
Cumarinas
/
Mycobacterium tuberculosis
/
Antituberculosos
Límite:
Animals
Idioma:
En
Revista:
Future Med Chem
Año:
2020
Tipo del documento:
Article
País de afiliación:
Brasil