Natural product derivatives with bactericidal activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis

作者：Phillips Joshua B; Smith Adrienne E; Kusche Brian R; Bessette Bradley A Jr; Swain P Whitney III; Bergmeier Stephen C; McMills Mark C; Wright Dennis L; Priestley Nigel D^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(19): 5936-5938.

DOI：10.1016/j.bmcl.2010.06.146

• Antibiotic
• Biosynthesis
• Nonactin
• Triazoloester

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.

• 出版日期2010-10-1