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Selective trihydroxyazepane NagZ inhibitors increase sensitivity of Pseudomonas aeruginosa to β-lactams
Author(s) -
Martine Mondon,
Soo Hur,
Grishma Vadlamani,
Prerana Rodrigues,
Polina Tsybina,
Antonio Oliver,
Brian L. Mark,
David J. Vocadlo,
Yves Blériot
Publication year - 2013
Publication title -
chemical communications
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.837
H-Index - 333
eISSN - 1364-548X
pISSN - 1359-7345
DOI - 10.1039/c3cc46646a
Subject(s) - pseudomonas aeruginosa , microbiology and biotechnology , antibiotics , bacteria , lactam , chemistry , gram negative bacteria , biology , stereochemistry , escherichia coli , biochemistry , gene , genetics
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.

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