Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 5, Pages 1767-1770Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.036
Keywords
Wall teichoic acids (WTAs); Staphylococcus aureus; Antibiotic; Bacteriostatic; Structure-activity relationship (SAR); Triazoloquinazoline; Targocil
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Funding
- NIH [1P01AI083214, 5R01GM078477, F32AI084316, F3178727]
- National Screening Laboratory for the Regional Centers of Excellence in Bio-defense and Emerging Infectious Diseases (NIAID) [U54 AI057159]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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