发明名称 OPTICAL MOLECULAR SENSORS FOR CYTOCHROME P450 ACTIVITY
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 (-OCR<2>H)p-, wherein for each p, all R<2> 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, R<2> is hydrogen, and Q is the ether form of a phenoxide fluorophore.
申请公布号 WO0035900(A1) 申请公布日期 2000.06.22
申请号 WO1999US29439 申请日期 1999.12.10
申请人 AURORA BIOSCIENCES CORPORATION 发明人 MAKINGS, LEWIS;ZLOKARNIK, GREGOR
分类号 G01N37/00;A61K45/00;A61P43/00;C07D219/06;C07D265/38;C07D311/16;C07D311/82;C07D493/10;C12Q1/26;(IPC1-7):C07D311/16 主分类号 G01N37/00
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