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    • 18. 发明申请
    • Novel antibacterial agents
    • 新型抗菌剂
    • US20090111737A1
    • 2009-04-30
    • US12082666
    • 2008-04-11
    • Burton G. ChristensenEdmund J. MoranJohn H. GriffinJ. Kevin JudiceYongQi MuJohn L. PaceMathai MammenJames Aggen
    • Burton G. ChristensenEdmund J. MoranJohn H. GriffinJ. Kevin JudiceYongQi MuJohn L. PaceMathai MammenJames Aggen
    • A61K38/14C07K7/00A61P43/00
    • C07D477/12C07D499/32C07D499/44C07D501/56
    • 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.
    • 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。