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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; Blackledge, Meghan S.; Lindsey, Erick A.; Minrovic, Bradley M.; Ackart, David F.; Jeon, Albert B.; Obregón ‐ Henao, Andrés; Melander, Roberta J.; Basaraba, Randall J.; Melander, Christian
- 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
BENZIMIDAZOLE derivatives; BETA lactam antibiotics; MYCOBACTERIUM smegmatis; MYCOBACTERIUM tuberculosis; BETA-lactamase inhibitors; MULTIDRUG resistance in bacteria
- Publication
Angewandte Chemie, 2017, Vol 129, Issue 14, p3998
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201612006