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Stability of Novel Siderophore Cephalosporin S-649266 against Clinically Relevant Carbapenemases
Author(s) -
Tsukasa Ito-Horiyama,
Yoshikazu Ishii,
Akinobu Ito,
Takafumi Sato,
Rio Nakamura,
Norio Fukuhara,
Masakatsu Tsuji,
Yoshinori Yamano,
Keizo Yamaguchi,
Kazuhiro Tateda
Publication year - 2016
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.03098-15
Subject(s) - meropenem , cephalosporin , hydrolysis , carbapenem , siderophore , chemistry , microbiology and biotechnology , nuclear chemistry , antibiotics , biology , biochemistry , antibiotic resistance , gene
To better understand the antibacterial activity of S-649266 against carbapenemase producers, its stability against clinically relevant carbapenemases was investigated. The catalytic efficiencies (k cat /Km ) of IMP-1, VIM-2, and L1 for S-649266 were 0.0048, 0.0050, and 0.024 μM−1 s−1 , respectively, which were more than 260-fold lower than that for meropenem. Only slight hydrolysis of S-649266 against KPC-3 was observed. NDM-1 hydrolyzed meropenem 3-fold faster than S-649266 at 200 μM.

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