Rapid Identification of Antibacterial Agents Effective against Staphylococcus aureus Using Small-Molecule Macroarrays
| Autor: | Helen E. Blackwell, Joseph R. Stringer, Matthew D. Bowman, Jennifer C. O'Neill |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Visualization methods
CHEMBIOL Staphylococcus aureus Pyridines Chemistry Pharmaceutical Clinical Biochemistry Microbial Sensitivity Tests Drug resistance Biology 010402 general chemistry medicine.disease_cause 01 natural sciences Biochemistry Microbiology Minimum inhibitory concentration Chalcones Drug Resistance Bacterial Drug Discovery medicine MICROBES Molecular Biology Pathogen Pharmacology 010405 organic chemistry General Medicine Small molecule Combinatorial chemistry Anti-Bacterial Agents 0104 chemical sciences Rapid identification Pyrimidines Drug Design Mic values Molecular Medicine Methicillin Resistance |
| Zdroj: | Chemistry & Biology. 14:351-357 |
| ISSN: | 1074-5521 |
| DOI: | 10.1016/j.chembiol.2007.03.006 |
| Popis: | SummaryThere is an urgent, global need for the development of new antibacterial agents. We have applied the small-molecule macroarray approach to the synthesis and screening of antibacterial compounds active against the Gram-positive pathogen Staphylococcus aureus. Several macroarrays of 1,3-diphenyl-2-propen-1-ones (chalcones), cyanopyridines, and pyrimidines were synthesized on a planar cellulose support system on the order of days. This support system was found to be highly compatible with antibacterial assay formats, including disk-diffusion and agar-overlay visualization methods. Further, sufficient compound was isolated from each spot of the macroarray for both compound characterization and minimum inhibitory concentration (MIC) estimation. Analysis of the small-molecule macroarrays in these assays uncovered a set of antibacterial agents with in vitro MIC values against methicillin-resistant S. aureus comparable to certain antibacterial drugs in use today. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|