Rapid identification of antibacterial compounds against Staphylococcus aureus using small molecule macroarrays

ORGN 634

Joseph R. Stringer, jstringer@wisc.edu, Matthew D. Bowman, mdbowman@wisc.edu, Jennifer C. O'Neill, oneill2@wisc.edu, and Helen E. Blackwell, blackwell@chem.wisc.edu. Department of Chemistry, University of Wisconsin-Madison, 1101 University Ave., Madison, WI 53706
Antibacterial resistance continues to be a global health concern today, emphasizing the need for the discovery of new antibacterial agents. We report the construction and characterization of a number of antibacterial small molecules active against methicillin-resistant Staphylococcus aureus (MRSA). Macroarrays of 1,3-diphenyl-2-propen-1-ones (chalcones) and cyanopyridine derivatives were synthesized on planar cellulose support derivatized with a Rink linker. Sufficient compound was isolated from each spot of the macroarray for both characterization and preliminary minimum inhibitory concentration (MIC) values. Analysis of these data reveals a set of antibacterial agents with novel structures and activities against MRSA that are comparable to antibacterial drugs in use today.