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    • 5. 发明申请
    • FLUORESCENT SUBSTRATES FOR DETECTING ORGANOPHOSPHATASE ENZYME ACTIVITY
    • 用于检测有机磷酸酶酶活性的荧光底物
    • WO2004094658A2
    • 2004-11-04
    • PCT/US2004/007897
    • 2004-03-16
    • AMERICAN RED CROSSSOUKHAREV, SergueiHAMMOND, David
    • SOUKHAREV, SergueiHAMMOND, David
    • C12Q1/42
    • C07F9/65522C07F9/6561C12Q1/42
    • Disclosed are compounds of the formula (I): wherein R 3 , R 4 , R 5 , R 9 , and R 10 are selected from the group consisting of H and groups or atoms other than H, and R 6 and R 8 are halo or hydrogen; X 1 , X 2 , and X 3 are independently O or S; provided that R 9 and R 10 are not simultaneously H, when all of X 1 , X 2 , and X 3 are O; and of the formula (II) wherein R 11 -R 14 are selected from the group consisting of H and groups or atoms other than H; X 4 - X 9 are independently O or S; n and m are 0 or 1 but m and n cannot be 0 simultaneously; R 15 - R 24 can be H or any substituent so long as the compound of formula II upon hydrolysis provides a fluorescent compound. These compounds are useful as substrates with high specificity for organophosphatase particularly human paraoxonase and bacterial organophosphorus hydrolase. Also disclosed is a method for detecting and/or measuring the paraoxonase activity in a fluid comprising contacting the fluid with a fluorescent substrate and measuring the fluorescence of the fluorescent product formed.
    • 公开了式(I)的化合物:其中R 3,R 4,R 5,R 9和R 10选自H和除 H和R 6和R 8是卤素或氢; X 1,X 2和X 3独立地为O或S; 条件是当R 1和X 3都全部为O时,R 9和R 10不同时为H; 和式(II)的化合物,其中R 11 -R 14选自H和H以外的基团或原子; X 4 - X 9独立地为O或S; n和m是0或1,但m和n不能同时为0; R 15 -R 24可以是H或任何取代基,只要在水解时式II化合物提供荧光化合物即可。 这些化合物可用作对有机磷酸酶特别是人类对氧磷酶和细菌有机磷水解酶具有高特异性的底物。 还公开了一种用于检测和/或测量流体中对氧磷酶活性的方法,包括使流体与荧光底物接触并测量形成的荧光产物的荧光。