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Infectious disease

Bacterial infection

FabI enoyl-(acyl carrier protein) reductase

Mouse and in vitro studies suggest a 4-pyridone fabI inhibitor could help treat Gram-positive and Gram-negative bacterial infections. Crystal structures of a narrow-spectrum, pyridone-based fabI inhibitor in complex with fabI from Staphylococcus aureus and Escherichia coli were used to rationally design a 4-pyridone fabI inhibitor. In a panel of bacterial cell cultures, the 4-pyridone fabI inhibitor showed an extended spectrum of bactericidal activity compared with the narrow-spectrum inhibitor. In a mouse model of MRSA infection, the 4-pyridone fabI inhibitor decreased infection compared with the generic, methicillin-based antibiotic oxacillin. Next steps include developing fabI inhibitors with further improvements in potency and spectrum of activity.

SciBX 7(19); doi:10.1038/scibx.2014.560
Published online May 15, 2014

Compounds covered by filed and pending patents; available for licensing from the Research Foundation for SUNY

Schiebel, J. et al. J. Biol. Chem.; published online April 16, 2014;
Contact: Caroline Kisker, University of Wuerzburg, Wuerzburg, Germany
Contact: Peter J. Tonge, Stony Brook University, Stony Brook, N.Y.