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Rhodanine hydrolysis leads to potent thioenolate mediated metallo-β-lactamase inhibition.

Abstract:

The use of β-lactam antibiotics is compromised by resistance, which is provided by β-lactamases belonging to both metallo (MBL)- and serine (SBL)-β-lactamase subfamilies. The rhodanines are one of very few compound classes that inhibit penicillin-binding proteins (PBPs), SBLs and, as recently reported, MBLs. Here, we describe crystallographic analyses of the mechanism of inhibition of the clinically relevant VIM-2 MBL by a rhodanine, which reveal that the rhodanine ring undergoes hydrolysis t...

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Publication status:
Published

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Publisher copy:
10.1038/nchem.2110

Authors


van Berkel, SS More by this author
Rydzik, AM More by this author
Avison, MB More by this author
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Publisher:
Nature Publishing Group
Journal:
Nature chemistry
Volume:
6
Issue:
12
Pages:
1084-1090
Publication date:
2014-12-05
DOI:
EISSN:
1755-4349
ISSN:
1755-4330
URN:
uuid:d6263a30-020e-4184-a313-fa1486a947c0
Source identifiers:
491754
Local pid:
pubs:491754
Language:
English

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