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Structure activity relationship studies on rhodanines and derived enethiol inhibitors of metallo-β-lactamases

Abstract:

Metallo-β-lactamases (MBLs) enable bacterial resistance to almost all classes of β-lactam antibiotics. We report studies on enethiol containing MBL inhibitors, which were prepared by rhodanine hydrolysis. The enethiols inhibit MBLs from different subclasses. Crystallographic analyses reveal that the enethiol sulphur displaces the di-Zn(II) ion bridging ‘hydrolytic’ water. In some, but not all, cases biophysical analyses provide evidence that rhodanine/enethiol inhibition involves formation of...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmc.2018.02.043

Authors


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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry; Organic Chemistry
Role:
Author
University of Oxford Clarendon Fund More from this funder
Diamond Light Source More from this funder
Publisher:
Elsevier Publisher's website
Journal:
Bioorganic and Medicinal Chemistry Journal website
Volume:
26
Issue:
11
Pages:
2928-2936
Publication date:
2018-02-23
Acceptance date:
2018-02-22
DOI:
EISSN:
1464-3391
ISSN:
0968-0896
Pmid:
29655609
Language:
English
Keywords:
Pubs id:
pubs:843427
UUID:
uuid:ec1e9896-f66f-4f04-be6f-cf2c34f5bb80
Local pid:
pubs:843427
Deposit date:
2018-05-03

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