Abstract
LY191145 is the prototype of a series of compounds with activities against vancomycin-resistant enterococci derived by modification of the glycopeptide antibiotic LY264826. LY191145 had MICs for vancomycin- and teicoplanin-resistant enterococci of < or = 4 micrograms/ml for 50% of isolates and < or = 16 micrograms/ml for 90% of isolates. Its MICs for vancomycin-resistant, teicoplanin-susceptible enterococci were 1 to 8 micrograms/ml. LY191145 retains the potent activities of its parent compound against staphylococci and streptococci. In vivo studies in a mouse infection model confirmed these activities. This compound indicates the potential of semisynthetic glycopeptides as agents against antibiotic-resistant gram-positive bacteria.
MeSH terms
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Animals
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Anti-Bacterial Agents / pharmacokinetics
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Anti-Bacterial Agents / pharmacology*
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Anti-Bacterial Agents / therapeutic use
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Drug Resistance, Microbial
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Enterococcus / drug effects*
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Enterococcus faecalis / drug effects
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Enterococcus faecium / drug effects
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacterial Infections / drug therapy
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Gram-Positive Bacterial Infections / microbiology
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Humans
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Male
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Methicillin Resistance
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Mice
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Microbial Sensitivity Tests
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Rats
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Rats, Sprague-Dawley
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Staphylococcus / drug effects
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Streptococcus / drug effects
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Vancomycin / analogs & derivatives
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Vancomycin / pharmacokinetics
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Vancomycin / pharmacology*
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Vancomycin / therapeutic use
Substances
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Anti-Bacterial Agents
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LY 191145
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Vancomycin