Natural product derivatives with bactericidal activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis
✍ Scribed by Joshua B. Phillips; Adrienne E. Smith; Brian R. Kusche; Bradley A. Bessette Jr.; P. Whitney Swain III; Stephen C. Bergmeier; Mark C. McMills; Dennis L. Wright; Nigel D. Priestley
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 337 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
We have shown that the intentional engineering of a natural product biosynthesis pathway is a useful way to generate stereochemically complex scaffolds for use in the generation of combinatorial libraries that capture the structural features of both natural products and synthetic compounds. Analysis of a prototype library based upon nonactic acid lead to the discovery of triazole-containing nonactic acid analogs, a new structural class of antibiotic that exhibits bactericidal activity against drug resistant, Gram-positive pathogens including Staphylococcus aureus and Enterococcus faecalis.