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Selective trihydroxyazepane NagZ inhibitors increase sensitivity of Pseudomonas aeruginosa to β-lactams.
- Source :
-
Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2013 Dec 04; Vol. 49 (93), pp. 10983-5. - Publication Year :
- 2013
-
Abstract
- AmpC β-lactamase confers resistance to β-lactam antibiotics in many Gram negative bacteria. Inducible expression of AmpC requires an N-acetylglucosaminidase termed NagZ. Here we describe the synthesis and characterization of hydroxyazepane inhibitors of NagZ. We find that these inhibitors enhance the susceptibility of clinically relevant Pseudomonas aeruginosa to β-lactams.
- Subjects :
- Acetylglucosaminidase metabolism
Anti-Bacterial Agents pharmacology
Azepines pharmacology
Bacterial Proteins metabolism
Binding Sites
Catalytic Domain
Crystallography, X-Ray
Drug Resistance, Bacterial drug effects
Enzyme Inhibitors pharmacology
Hydrogen Bonding
Pseudomonas aeruginosa drug effects
beta-Lactamases metabolism
beta-Lactams pharmacology
Acetylglucosaminidase antagonists & inhibitors
Anti-Bacterial Agents chemistry
Azepines chemistry
Bacterial Proteins antagonists & inhibitors
Enzyme Inhibitors chemistry
Pseudomonas aeruginosa enzymology
beta-Lactams chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1364-548X
- Volume :
- 49
- Issue :
- 93
- Database :
- MEDLINE
- Journal :
- Chemical communications (Cambridge, England)
- Publication Type :
- Academic Journal
- Accession number :
- 24136176
- Full Text :
- https://doi.org/10.1039/c3cc46646a