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- Title
The Discovery of 2-Aminobenzimidazoles That Sensitize Mycobacterium smegmatis and M. tuberculosis to β-Lactam Antibiotics in a Pattern Distinct from β-Lactamase Inhibitors.
- Authors
Nguyen, T. Vu; Lindsey, Erick A.; Minrovic, Bradley M.; Melander, Roberta J.; Melander, Christian; Blackledge, Meghan S.; Ackart, David F.; Jeon, Albert B.; Obregón-Henao, Andrés; Basaraba, Randall J.
- Abstract
A library of 2-aminobenzimidazole derivatives was screened for the ability to suppress β-lactam resistance in Mycobacterium smegmatis. Several non-bactericidal compounds were identified that reversed intrinsic resistance to β-lactam antibiotics in a manner distinct from β-lactamase inhibitors. Activity also translates to M. tuberculosis, with a lead compound from this study potently suppressing carbenicillin resistance in multiple M. tuberculosis strains (including multidrug-resistant strains). Preliminary mechanistic studies revealed that the lead compounds act through a mechanism distinct from that of traditional β-lactamase inhibitors.
- Subjects
BENZIMIDAZOLES; MYCOBACTERIUM smegmatis; MYCOBACTERIUM tuberculosis; BETA-lactamase inhibitors; ANTIBIOTICS
- Publication
Angewandte Chemie International Edition, 2017, Vol 56, Issue 14, p3940
- ISSN
1433-7851
- Publication type
Article
- DOI
10.1002/anie.201612006