| pubmed-article:18443106 | rdf:type | pubmed:Citation | lld:pubmed |
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| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0025952 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0038402 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0038170 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0020205 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0220825 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C2603343 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C2003903 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:18443106 | lifeskim:mentions | umls-concept:C2603496 | lld:lifeskim |
| pubmed-article:18443106 | pubmed:issue | 7 | lld:pubmed |
| pubmed-article:18443106 | pubmed:dateCreated | 2008-6-25 | lld:pubmed |
| pubmed-article:18443106 | pubmed:abstractText | We present data from antimicrobial assays performed in vitro that pertain to the potential clinical utility of a novel rifamycin-quinolone hybrid antibiotic, CBR-2092, for the treatment of infections mediated by gram-positive cocci. The MIC(90)s for CBR-2092 against 300 clinical isolates of staphylococci and streptococci ranged from 0.008 to 0.5 mug/ml. Against Staphylococcus aureus, CBR-2092 exhibited prolonged postantibiotic effects (PAEs) and sub-MIC effects (SMEs), with values of 3.2, 6.5, and >8.5 h determined for the PAE (3x MIC), SME (0.12x MIC), and PAE-SME (3x MIC/0.12x MIC) periods, respectively. Studies of genetically defined mutants of S. aureus indicate that CBR-2092 is not a substrate for the NorA or MepA efflux pumps. In minimal bactericidal concentration and time-kill studies, CBR-2092 exhibited bactericidal activity against staphylococci that was retained against rifampin- or intermediate quinolone-resistant strains, with apparent paradoxical cidal characteristics against rifampin-resistant strains. In spontaneous resistance studies, CBR-2092 exhibited activity consistent with balanced contributions from its composite pharmacophores, with a mutant prevention concentration of 0.12 mug/ml and a resistance frequency of <10(-12) determined at 1 mug/ml in agar for S. aureus. Similarly, CBR-2092 suppressed the emergence of preexisting rifamycin resistance in time-kill studies undertaken at a high cell density. In studies of the intracellular killing of S. aureus, CBR-2092 exhibited prolonged bactericidal activity that was superior to the activities of moxifloxacin, rifampin, and a cocktail of moxifloxacin and rifampin. Overall, CBR-2092 exhibited promising activity in a range of antimicrobial assays performed in vitro that pertain to properties relevant to the effective treatment of serious infections mediated by gram-positive cocci. | lld:pubmed |
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| pubmed-article:18443106 | pubmed:language | eng | lld:pubmed |
| pubmed-article:18443106 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18443106 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:18443106 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:18443106 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:18443106 | pubmed:issn | 1098-6596 | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:OnoKK | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:LynchA... | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:RobertsonGreg... | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:DuncanLeonard... | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:RocheEric DED | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:MorrisTimothy... | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:YanDalaiD | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:DoyleTimothy... | lld:pubmed |
| pubmed-article:18443106 | pubmed:author | pubmed-author:BonventreEric... | lld:pubmed |
| pubmed-article:18443106 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:18443106 | pubmed:volume | 52 | lld:pubmed |
| pubmed-article:18443106 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:18443106 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:18443106 | pubmed:pagination | 2324-34 | lld:pubmed |
| pubmed-article:18443106 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:18443106 | pubmed:meshHeading | pubmed-meshheading:18443106... | lld:pubmed |
| pubmed-article:18443106 | pubmed:year | 2008 | lld:pubmed |
| pubmed-article:18443106 | pubmed:articleTitle | In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: microbiology profiling studies with staphylococci and streptococci. | lld:pubmed |
| pubmed-article:18443106 | pubmed:affiliation | Cumbre Pharmaceuticals Inc., 1502 Viceroy Drive, Dallas, TX 75235-2304, USA. | lld:pubmed |
| pubmed-article:18443106 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:18443106 | pubmed:publicationType | In Vitro | lld:pubmed |
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