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  • Title: Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.
    Author: Mitton-Fry MJ, Brickner SJ, Hamel JC, Barham R, Brennan L, Casavant JM, Ding X, Finegan S, Hardink J, Hoang T, Huband MD, Maloney M, Marfat A, McCurdy SP, McLeod D, Subramanyam C, Plotkin M, Reilly U, Schafer J, Stone GG, Uccello DP, Wisialowski T, Yoon K, Zaniewski R, Zook C.
    Journal: Bioorg Med Chem Lett; 2017 Aug 01; 27(15):3353-3358. PubMed ID: 28610977.
    Abstract:
    Novel (non-fluoroquinolone) inhibitors of bacterial type II topoisomerases (NBTIs) are an emerging class of antibacterial agents. We report an optimized series of cyclobutylaryl-substituted NBTIs. Compound 14 demonstrated excellent activity both in vitro (S. aureus MIC90=0.125μg/mL) and in vivo (systemic and tissue infections). Enhanced inhibition of Topoisomerase IV correlated with improved activity in S. aureus strains with mutations conferring resistance to NBTIs. Compound 14 also displayed an improved hERG IC50 of 85.9μM and a favorable profile in the anesthetized guinea pig model.
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