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  • Title: Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.
    Author: Miles TJ, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Rittenhouse S, Xiang H, Pearson N.
    Journal: Bioorg Med Chem Lett; 2011 Dec 15; 21(24):7483-8. PubMed ID: 22030032.
    Abstract:
    As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via inhibition of bacterial topoisomerases II and IV. We have investigated various subunits in this series and report advanced studies on compound 7 which demonstrates good PK and in vivo efficacy properties.
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