Rapid identification of antibacterial agents effective against Staphylococcus aureus using small-molecule macroarrays |
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Authors: | Bowman Matthew D O'Neill Jennifer C Stringer Joseph R Blackwell Helen E |
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Institution: | Department of Chemistry, University of Wisconsin, Madison, 1101 University Avenue, Madison, WI 53706, USA. |
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Abstract: | There 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. |
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