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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2011-7-1
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pubmed:abstractText |
The preparation and characterization of a series of thiophenyl oxime phosphonate beta-lactamase inhibitors is described. A number of these analogs were potent and selective inhibitors of class C beta-lactamases from Pseudomonas aeruginosa and Enterobacter cloacae. Compounds 3b and 7 reduced the MIC of imipenem against an AmpC expressing strain of imipenem-resistant P. aeruginosa. A number of the title compounds retained micromolar potency against the class D OXA-40 beta-lactamase from Acinetobacter baumannii and at high concentrations compound 3b was shown to reduce the MIC of imipenem against a highly imipenem-resistant strain of A. baumanii expressing the OXA-40 beta-lactamase. In mice compound 3b exhibited phamacokinetics similar to imipenem.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4363-5
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pubmed:meshHeading |
pubmed-meshheading:21664132-Acinetobacter baumannii,
pubmed-meshheading:21664132-Anti-Bacterial Agents,
pubmed-meshheading:21664132-Drug Resistance, Bacterial,
pubmed-meshheading:21664132-Enzyme Inhibitors,
pubmed-meshheading:21664132-Imipenem,
pubmed-meshheading:21664132-Microbial Sensitivity Tests,
pubmed-meshheading:21664132-Oximes,
pubmed-meshheading:21664132-Phosphonic Acids,
pubmed-meshheading:21664132-Pseudomonas aeruginosa,
pubmed-meshheading:21664132-Thiophenes,
pubmed-meshheading:21664132-beta-Lactamases
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pubmed:year |
2011
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pubmed:articleTitle |
Thiophenyl oxime-derived phosphonates as nano-molar class C beta-lactamase inhibitors reducing MIC of imipenem against Pseudomonas aeruginosa and Acinetobacter baumannii.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck & Co., Inc., Rahway, NJ 07065, USA. qiang_tan@merck.com
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pubmed:publicationType |
Journal Article
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