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The discovery of a novel siderophore cephalosporin Cefiderocol
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- Aoki Toshiaki
- CMC R&D Division, SHIONOGI & CO., LTD.
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- Yamawaki Kenji
- Laboratory for Medicinal Chemistry Research, Pharmaceutical Research Division, SHIONOGI & CO., LTD.
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- Sato Takafumi
- Pharmaceutical Research Division, SHIONOGI & CO., LTD.
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- Nishitani Yasuhiro
- SHIONOGI & CO., LTD.
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- Yamano Yoshinori
- Pharmaceutical Research Division, SHIONOGI & CO., LTD.
Bibliographic Information
- Other Title
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- 新規シデロフォアセファロスポリン抗菌薬 セフィデロコル（Cefiderocol）の創製
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Description
The threat of carbapenem resistant Gram-negative pathogens e.g. Enterobacterales, P. aeruginosa and A. baumannii is expanding worldwide. One strategy to discover a new antibacterial to be active against these resistant pathogens is to utilize the bacterial iron acquisition system by attaching a siderophore-mimicking molecule to the parent molecule. In 1980’s, our team identified a siderophore cephalosporin A-2, which displayed a potent activity against P. aeruginosa. We restarted the SAR study of siderophore cephalosporin to increase the in vitro and in vivo antimicrobial activity against various carbapenemase-producing resistant strains by the modification of the C-3 and C-7 side chains of A-2. Here, we report the SAR results about the several siderophore cephalosporins that led to the discovery of Cefiderocol.
Journal
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- MEDCHEM NEWS
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MEDCHEM NEWS 31 (2), 75-80, 2021-05-01
The Pharmaceutical Society of Japan
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Keywords
Details 詳細情報について
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- CRID
- 1390850857223387008
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- NII Article ID
- 130008033653
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- ISSN
- 24328626
- 24328618
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- Text Lang
- ja
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- Data Source
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- JaLC
- CiNii Articles
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- Abstract License Flag
- Disallowed
