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Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase

Abstract:

A paucity of novel acting antibacterials is in development to treat the rising threat of antimicrobial resistance, particularly in Gram-negative hospital pathogens, which has led to renewed efforts in antibiotic drug discovery. Fluoroquinolones are broad-spectrum antibacterials that target DNA gyrase by stabilizing DNA-cleavage complexes, but their clinical utility has been compromised by resistance. We have identified a class of antibacterial thiophenes that target DNA gyrase with a unique m...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1073/pnas.1700721114

Authors


Thalji, RK More by this author
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Grant:
Joint Undertaking under Grant Agreement 115583
Publisher:
National Academy of Sciences Publisher's website
Journal:
Proceedings of the National Academy of Sciences Journal website
Volume:
114
Issue:
22
Pages:
E4492-E4500
Publication date:
2017-05-15
DOI:
EISSN:
1091-6490
ISSN:
0027-8424
Pubs id:
pubs:695746
URN:
uri:5ee9c29d-63e1-41c8-b496-d45d1f4900ef
UUID:
uuid:5ee9c29d-63e1-41c8-b496-d45d1f4900ef
Local pid:
pubs:695746
Language:
English
Keywords:

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