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Novel semisynthetic derivative of antibiotic eremomycin active against drug-resistant gram-positive pathogens including Bacillus anthracis

Journal of Medicinal Chemistry, ISSN: 0022-2623, Vol: 50, Issue: 15, Page: 3681-3685
2007
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Article Description

Five adamantyl-containing carboxamides of eremomycin or vancomycin were synthesized and their antibacterial activities against some Gram-positive clinical isolates were investigated in vitro and in vivo. The adamantyl-2 amide of glycopeptide antibiotic eremomycin (1a in Chart 1, AN0900) was the most active compound and showed high activity against several Gram-positive pathogens: vancomycin-susceptible staphylococci and enterococci, glycopeptide-intermediate-resistant Staphylococcus aureus, and glycopeptide-resistant enterococci. Compound 1a was equally active in vitro against both Ciprofloxacin-susceptible and -resistant Bacillus anthracis strains (MICs 0.25-0.5 μg/mL). It was distinguished by having a 2.8 h half-life (t) in mice and a volume of distribution of 2.18 L/kg. Compound 1a was active against Staphylococcus aureus in mice (iv) and provided complete protection against a lethal intravenous challenge with vegetative B. anthracis bacilli and also in a murine pulmonary anthrax model in which mice were challenged with Bacillus anthracis spores. © 2007 American Chemical Society.

Bibliographic Details

Maples, Kirk R; Wheeler, Conrad; Ip, Emily; Plattner, Jacob J; Chu, Daniel; Zhang, Yong-Kang; Preobrazhenskaya, Maria N; Printsevskaya, Svetlana S; Solovieva, Svetlana E; Olsufyeva, Evgenia N; Heine, Henry; Lovchik, Julie; Lyons, C Richard

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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