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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2003-8-7
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pubmed:abstractText |
Novel quinolone antibacterial agents bearing (3S)-amino-(4R)-ethylpiperidines were designed by using low energy conformation analysis and synthesized by applying a conventional coupling reaction of the quinolone nuclei with new piperidine side chains. These compounds were tested in MIC assays and found to be highly potent against Gram-positive and Gram-negative organisms. In particular, the new compounds exhibited high activity against the resistant pathogens Staphylococcus aureus (MRCR) and Streptococcus pneumoniae (PR). Importantly, when the (3S)-amino-(4R)-ethylpiperidinyl quinolones were compared with marketed quinolones sharing the same quinolone nuclei but different side chains at the C-7 position, the new quinolones showed superior activity against Gram-positive organisms, including resistant pathogens.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3655-61
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:12904069-Anti-Bacterial Agents,
pubmed-meshheading:12904069-Bacteria,
pubmed-meshheading:12904069-DNA, Superhelical,
pubmed-meshheading:12904069-DNA Gyrase,
pubmed-meshheading:12904069-Drug Resistance, Bacterial,
pubmed-meshheading:12904069-Escherichia coli,
pubmed-meshheading:12904069-Gram-Negative Bacteria,
pubmed-meshheading:12904069-Gram-Positive Bacteria,
pubmed-meshheading:12904069-Microbial Sensitivity Tests,
pubmed-meshheading:12904069-Models, Molecular,
pubmed-meshheading:12904069-Molecular Conformation,
pubmed-meshheading:12904069-Piperidines,
pubmed-meshheading:12904069-Quinolones,
pubmed-meshheading:12904069-Stereoisomerism,
pubmed-meshheading:12904069-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
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pubmed:affiliation |
Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, Ohio 45040, USA. hu.xe@pg.com
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pubmed:publicationType |
Journal Article
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