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    Pyrazolopyrimidine antibacterial agents
    3.
    发明授权
    Pyrazolopyrimidine antibacterial agents 有权

    公开(公告)号：US10155766B2

    公开(公告)日：2018-12-18

    申请号：US15611512

    申请日：2017-06-01

    申请人： BOARD OF TRUSTEES OF NORTHERN ILLINOIS UNIVERSITY

    发明人： Timothy J. Hagen ,  Joy M. Blain ,  Gashaw M. Goshu ,  Brian E. Hartnett

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06

    摘要： Pyrazolopyrimidine compounds for inhibition of isoprenoid biosynthesis have a formula (I) or a pharmaceutically acceptable salt thereof. In formula (I), R1 includes an alkyl group and R2 includes an optionally substituted moiety selected from the group consisting of an optionally substituted benzyl group, an optionally substituted phenethyl group, an optionally substituted ethanol group, an optionally substituted ethyl acetate group, an optionally substituted methyl furan group, an optionally substituted 3-ethyl indole group, and a lower alkyl group. Compositions containing pyrazolopyrimidine compounds and methods for using pyrazolopyrimidine compounds are described.

    OXADIAZOLE AND PHENOL DERIVATIVES AS ANTIBACTERIAL AND/OR HERBICIDAL AGENTS
    5.
    发明申请
    OXADIAZOLE AND PHENOL DERIVATIVES AS ANTIBACTERIAL AND/OR HERBICIDAL AGENTS 审中-公开

    公开(公告)号：US20180271098A1

    公开(公告)日：2018-09-27

    申请号：US15933608

    申请日：2018-03-23

    申请人： BOARD OF TRUSTEES OF NORTHERN ILLINOIS UNIVERSITY

    发明人： Timothy J. Hagen ,  Michael Thompson ,  Jeremy R. Troxell ,  Brian E. Hartnett

    IPC分类号： A01N43/82 ,  C07D413/04 ,  C07D417/04 ,  C07D209/12 ,  A01N43/36

    CPC分类号： A01N43/82 ,  A01N43/36 ,  C07D209/12 ,  C07D413/04 ,  C07D417/04

    摘要： Antimicrobial resistance is rising at an alarming rate. The methylerythritol phosphate (MEP) pathway is a metabolic pathway that produces the isoprenoids isopentyl pyrophosphate (IPP) and dimethylallyl pyrophosphate (DMAPP). Notably, the MEP pathway is present in bacteria and not mammals, which made the enzymes of the MEP pathway attractive targets for discovering new anti-infective agents due to reduced chances of off-target interactions leading to side effects. The biophysical properties of 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase (IspD) and 4-diphosphocytidyl-2-C-methyl-D-erythritol kinase (IspE) were determined to aid discovery of novel inhibitors. Thermal shift screening was used as an initial filter to narrow down a library of compounds with thermal shifts greater than 1° C., which could indicate binding to the IspD and IspE enzymes. Follow-up studies were performed using isothermal titration calorimetry and enzymatic inhibition assays. Results from these studies have revealed compounds with high micromolar inhibition of both IspD from Escherichia coli and IspE from Burkholderia thailandensis. The hit compounds are used for future development of more potent IspD and IspE inhibitors.