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    Optical molecular sensors for cytochrome P450 activity
    6.
    发明授权
    Optical molecular sensors for cytochrome P450 activity 有权
    用于细胞色素P450活性的光学分子传感器

    公开(公告)号：US08153828B2

    公开(公告)日：2012-04-10

    申请号：US12499047

    申请日：2009-07-07

    申请人： Lewis Makings ,  Gregor Zlokarnik

    发明人： Lewis Makings ,  Gregor Zlokarnik

    IPC分类号： C07D311/06

    CPC分类号： C07D493/10 ,  C07D219/06 ,  C07D265/38 ,  C07D311/16 ,  C07D311/82 ,  C12Q1/26 ,  G01N2333/90245 ,  G01N2500/02 ,  Y10S435/968

    摘要： The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Q is a chemical moiety that gives rise to optical properties in its hydroxy or hyrdoxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form.

    摘要翻译： 本发明提供了可用作至少一种细胞色素P450酶的活性的光学探针或传感器的化合物，以及使用该化合物筛选候选药物的方法以及通过这些方法鉴定的候选药物。 本发明的光学探针是具有一般结构YLQ的化合物，其中Q是一种化学部分，其产生与其醚形式产生的光学性质不同的羟基或羟乙酸酯，苯酚或酚盐形式的光学性质 。

    OPTICAL MOLECULAR SENSORS FOR CYTOCHROME P450 ACTIVITY
    10.
    发明申请
    OPTICAL MOLECULAR SENSORS FOR CYTOCHROME P450 ACTIVITY 审中-公开

    公开(公告)号：US20070072256A1

    公开(公告)日：2007-03-29

    申请号：US11531136

    申请日：2006-09-12

    申请人： Lewis MAKINGS ,  Gregor ZLOKARNIK

    发明人： Lewis MAKINGS ,  Gregor ZLOKARNIK

    IPC分类号： C12Q1/26

    CPC分类号： C07D493/10 ,  C07D265/38 ,  C07D311/16 ,  C07D311/82 ,  C12Q1/26 ,  G01N2333/90245 ,  G01N2500/02

    摘要： The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Y is selected from the group consisting of Q as herein defined, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; L is selected from the group of (—OCR2H)p—, wherein for each p, all R2 are separately selected from the group consisting of a hydrogen atom, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and p is a positive integer no greater than twelve; and Q is a chemical moiety that gives rise to optical properties in its hydroxy or hydroxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form. Most preferably, p is one, R2 is hydrogen, and Q is the ether form of a phenoxide fluorophore.