The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents

…, E Ellsworth, S Hagen, M Huband, T Joannides…

Index: Murphy, Sean T.; Case, Heather L.; Ellsworth, Edmund; Hagen, Susan; Huband, Michael; Joannides, Themis; Limberakis, Chris; Marotti, Keith R.; Ottolini, Amy M.; Rauckhorst, Mark; Starr, Jeremy; Stier, Michael; Taylor, Clarke; Zhu, Tong; Blaser, Adrian; Denny, William A.; Lu, Guo-Liang; Smaill, Jeff B.; Rivault, Freddy Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 8 p. 2150 - 2155

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Citation Number: 40

Abstract

Several novel series of nitrile-containing fluoroquinolones with weakly basic amines are reported which have reduced potential for hERG (human ether-a-go-go gene) channel inhibition as measured by the dofetilide assay. The new fluoroquinolones are potent against both Gram-positive and fastidious Gram-negative strains, including Methicillin resistant Staphylococcus aureus and fluoroquinolone-resistant Streptococcus pneumoniae. ...