Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1767-1770
2010
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1767-1770
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.01.036Titel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_2844852
- Format
- –
- Schlagworte
- 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)