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    Novel antibacterial agents
    5.
    发明申请
    Novel antibacterial agents 审中-公开
    新型抗菌剂

    公开(公告)号：US20090111737A1

    公开(公告)日：2009-04-30

    申请号：US12082666

    申请日：2008-04-11

    申请人： Burton G. Christensen ,  Edmund J. Moran ,  John H. Griffin ,  J. Kevin Judice ,  YongQi Mu ,  John L. Pace ,  Mathai Mammen ,  James Aggen

    发明人： Burton G. Christensen ,  Edmund J. Moran ,  John H. Griffin ,  J. Kevin Judice ,  YongQi Mu ,  John L. Pace ,  Mathai Mammen ,  James Aggen

    IPC分类号： A61K38/14 ,  C07K7/00 ,  A61P43/00

    CPC分类号： C07D477/12 ,  C07D499/32 ,  C07D499/44 ,  C07D501/56

    摘要： This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

    摘要翻译： 本发明涉及作为抗菌剂的新型多结合化合物（试剂）。 本发明的多相结合化合物包含2-10个配体，其通过连接体或连接体共价连接，其中所述各单体（即，未连接）状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力 用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。 特别地，本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体，其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域，转肽酶，转肽酶的底物， β-内酰胺酶，pencillinase酶，头孢菌素酶，转糖基酶或转糖基酶酶底物; 优选地，配体选自β-内酰胺或糖肽类抗菌剂。