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pubmed-article:21664132pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:21664132pubmed:copyrightInfoCopyright © 2011 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:21664132pubmed:articleTitleThiophenyl oxime-derived phosphonates as nano-molar class C beta-lactamase inhibitors reducing MIC of imipenem against Pseudomonas aeruginosa and Acinetobacter baumannii.lld:pubmed
pubmed-article:21664132pubmed:affiliationDepartment of Medicinal Chemistry, Merck & Co., Inc., Rahway, NJ 07065, USA. qiang_tan@merck.comlld:pubmed
pubmed-article:21664132pubmed:publicationTypeJournal Articlelld:pubmed
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