Modulating the Spectrum of FabI Inhibition by Pyridones 1 Rational Design of Broad-Spectrum Antibacterial Activity based on a Clinically Relevant Enoyl-ACP Reductase Inhibitor *

Johannes Schiebel,Andrew Chang,Sonam Shah,Yang Lu,Li Liu,Pan Pan,Maria W. Hirschbeck, Mona Tareilus,Sandra Eltschkner,Weixuan Yu,Jason E. Cummings, Susan E. Knudson,Gopal R. Bommineni, Stephen G. Walker,Richard A. Slayden,Christoph A. Sotriffer,Peter J. Tonge,Caroline Kisker

semanticscholar（2014）

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摘要

Background: The FabI inhibitor CG400549 is a promising new anti-staphylococcal drug candidate with recently validated human efficacy. Results: We revealed the molecular determinants conferring S. aureus FabI selectivity to rationally design a compound with an improved antibacterial activity spectrum. Conclusion: The 4-pyridone PT166 represents a critical step towards Gram-negative and mycobacterial coverage. Significance: We provide an approach to expand the spectrum of antimicrobial activity. http://www.jbc.org/cgi/doi/10.1074/jbc.M113.532804 The latest version is at JBC Papers in Press. Published on April 16, 2014 as Manuscript M113.532804

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