Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus.
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.
The New England Regional Center of Excellence in Biodefense and Emerging Infectious Diseases (NERCE/BEID), Harvard Medical School, Boston, MA 02115, USA.
Kyungae
K
Lee
Jennifer
J
Campbell
Jonathan G
JG
Swoboda
Gregory D
GD
Cuny
Suzanne
S
Walker
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013682:Teichoic Acids / Q000096:biosynthesis* / Q000378:metabolism
D000900:Anti-Bacterial Agents; D011799:Quinazolines; D013682:Teichoic Acids