LIGHT ACTIVATED ACYL-ENZYMES
    4.
    发明公开
    LIGHT ACTIVATED ACYL-ENZYMES 失效
    活化的ACYL-酶

    公开(公告)号:EP0489836A4

    公开(公告)日:1993-05-26

    申请号:EP90913585

    申请日:1990-08-27

    申请人: DUKE UNIVERSITY

    摘要: Light activated acyl-enzymes of formula (III) are disclosed. In the compounds of formula (III) ENZ is an enzyme, X is O or S, Y is -NR3R4, -OR5, or -SR5, and Z is a nucleophile; m is 0 to 3 and n is 1 or 2; Y is substituted on the ring at either or both of the 4 and 6 position. R1 and R2 are each independently H, C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl. R3 and R4 are each independently H, C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl, except that R3 and R4 are not simultaneously both H. R5 is C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl. Methods of using the acyl-enzymes and intermediates for making the acyl-enzymes are disclosed. A preferred intermediate is 2-propenoic acid, 3-(2-hydroxy-4-diethylaminophenyl)-2-methyl-, 4-(aminoiminomethyl)phenyl ester, (E)-, monohydrochloride salt, which is preferably reacted with thrombin to form an acyl-thrombin.

    摘要翻译: 公开了式(III)的光活化酰基 - 酶。 在式(III)化合物中,ENZ是酶,X是O或S,Y是-NR3R4,-OR5或-SR5,并且Z是亲核试剂; m为0至3且n为1或2; Y在4位和6位中的任一个或两个上在环上被取代。 R1和R2各自独立地为H,C1-C4烷基,C3-C4非共轭烯基或C3-C4非共轭炔基。 R3和R4各自独立地为H,C1-C4烷基,C3-C4非共轭烯基或C3-C4非共轭炔基,除了R3和R4不同时为H。R5为C1-C4烷基,C3-C4非共轭烯基, 或C3至C4未连接的炔基。 公开了使用酰基 - 酶和中间体制备酰基 - 酶的方法。 优选的中间体是2-丙烯酸,3-(2-羟基-4-二乙基氨基苯基)-2-甲基 - ,4-(氨基亚氨基甲基)苯基酯,(E) - 一盐酸盐,其优选与凝血酶反应以形成 一种酰基凝血酶。