Rapid identification of antibacterial agents effective against Staphylococcus aureus using small-molecule macroarrays
Rapid identification of antibacterial agents effective against Staphylococcus aureus using small-molecule macroarrays
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DOI：
10.1016/j.chembiol.2007.03.006
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发表时间：
2007-04-01
影响因子：
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通讯作者：
Blackwell, Helen E.
中科院分区：
文献类型：
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作者：
Bowman, Matthew D.;O'Neill, Jennifer C.;Blackwell, Helen E.
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.
