Journal
JOURNAL OF ANTIBIOTICS
Volume 61, Issue 10, Pages 595-602Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/ja.2008.79
Keywords
multivalent; multivalency; bifunctional; beta-lactam; glycopeptide; antibiotic; MRSA
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The design, synthesis and antibacterial activity of novel glycopeptide/beta-lactam heterodimers is reported. Employing a multivalent approach to drug discovery, vancomycin and cephalosporin synthons, A and B respectively, were chemically linked to yield heterodimer antibiotics. These novel compounds were designed to inhibit Gram-positive bacterial cell wall biosynthesis by simultaneously targeting the principal cellular targets of both glycopeptides and beta-lactams. The antibiotics 8a similar to f displayed remarkable potency against a wide range of Gram-positive organisms including methicillin-resistant Staphylococcus aureus (MRSA). Compound 8e demonstrated excellent bactericidal activity against MRSA (ATCC 33591) and initial evidence supports a multivalent mechanism of action for this important new class of antibiotic.
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