Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus

The synthesis and biological evaluation of a focused library of wall teichoic acid biosynthesis inhibitors is reported. A small molecule (1835F03) that inhibits Staphylococcus aureus wall teichoic acid biosynthesis, a proposed antibiotic target, has been discovered. Rapid, parallel, solution-phase s...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1767-1770
Main Authors: Lee, Kyungae, Campbell, Jennifer, Swoboda, Jonathan G., Cuny, Gregory D., Walker, Suzanne
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotic
Antibiotics. Antiinfectious agents. Antiparasitic agents
Bacteriostatic
Biological and medical sciences
Medical sciences
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Quinazolines - chemical synthesis
Quinazolines - chemistry
Quinazolines - pharmacology
Staphylococcus aureus
Staphylococcus aureus - drug effects
Structure-Activity Relationship
Structure–activity relationship (SAR)
Targocil
Teichoic Acids - biosynthesis
Teichoic Acids - metabolism
Triazoloquinazoline
Wall teichoic acids (WTAs)
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Summary:The synthesis and biological evaluation of a focused library of wall teichoic acid biosynthesis inhibitors is reported. A small molecule (1835F03) that inhibits Staphylococcus aureus wall teichoic acid biosynthesis, a proposed antibiotic target, has been discovered. Rapid, parallel, solution-phase synthesis was employed to generate a focused library of analogs, providing detailed information about structure–activity relationships and leading to the identification of targocil, a potent antibiotic.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.036