4-oxazolidinone natural products, highlighted by lipoxazolidinone A, are unusual molecules isolated from marine sources.  Through rapid chemcial synthesis and medicinal chemistry/chemical biology efforts, we have demonstrated that these heterocycles are potent antimicrobial agents against a wide panel of drug resistant Gram-positive pathogens, and new derivatives also display activity against Gram-negative pathogens as well.  This talk will focus on our development of the molecular scaffold, optimization of the molecular properties and the study of the mechanism of action and generation of resistance.  Of great interest, these molecules possess a dual mechanism of action (cell well and protein synthesis inhibitors) and do not display significant toxicity to mammalian cells.  Further, resistance is slow to develop.

Development of 4-oxazolidinone natural products as infectious disease lead compounds

256th National Meeting (2018)

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