The Discovery of 2-Aminobenzimidazoles That Sensitize Mycobacterium smegmatis and M.â
tuberculosis to ß-Lactam Antibiotics in a Pattern Distinct from ß-Lactamase Inhibitors.
Angew Chem Int Ed Engl
; 56(14): 3940-3944, 2017 03 27.
Article
en En
| MEDLINE
| ID: mdl-28247991
ABSTRACT
A library of 2-aminobenzimidazole derivatives was screened for the ability to suppress ß-lactam resistance in Mycobacterium smegmatis. Several non-bactericidal compounds were identified that reversed intrinsic resistance to ß-lactam antibiotics in a manner distinct from ß-lactamase inhibitors. Activity also translates to M.â
tuberculosis, with a lead compound from this study potently suppressing carbenicillin resistance in multiple M.â
tuberculosis strains (including multidrug-resistant strains). Preliminary mechanistic studies revealed that the lead compounds act through a mechanism distinct from that of traditional ß-lactamase inhibitors.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Bencimidazoles
/
Mycobacterium smegmatis
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Inhibidores de beta-Lactamasas
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Lactamas
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Antibacterianos
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Mycobacterium tuberculosis
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Año:
2017
Tipo del documento:
Article
País de afiliación:
Estados Unidos