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    • 73. 发明申请
    • Novel Fluorescent Amino Acid Derivative and Production Method Of The Same
    • 新型荧光氨基酸衍生物及其制备方法
    • US20090240026A1
    • 2009-09-24
    • US12306784
    • 2007-07-03
    • Masumi TakiMasahiko Sisido
    • Masumi TakiMasahiko Sisido
    • C07K2/00C07D219/00
    • C07D219/06C09K11/06C09K2211/1029
    • An object of the present invention is to provide a novel fluorescent amino acid derivative which can be synthesized by simple steps, can be excited particularly by a blue laser ray region of visible light, and has an improved light stability. Another object is to provide a production method of the fluorescent amino acid derivative. These objects can be achieved by a fluorescent amino acid derivative which is an acridone derivative substituted with an amino acid to comprise an electrophilic substituent group between the amino acid and the acridone derivative. Instead of a conventional strategy that aminophenylalanine is used as a starting material to form a fluorescent group through a coupling reaction and an intramolecular cyclization reaction, a fluorescent acridone derivative is used as a starting material to furnish the material to a reactive group by a position-specific electrophilic substitution reaction, and then the acridone derivative having the reactive group is allowed to couple with an amino acid derivative.
    • 本发明的目的是提供可以通过简单的步骤合成的新的荧光氨基酸衍生物,特别可以通过可见光的蓝色激光射线区域被激发,并且具有改善的光稳定性。 另一个目的是提供荧光氨基酸衍生物的制备方法。 这些目的可以通过荧光氨基酸衍生物来实现,其是由氨基酸取代的吖啶酮衍生物,其在氨基酸和吖啶酮衍生物之间包含亲电取代基。 代替使用氨基苯丙氨酸作为通过偶联反应和分子内环化反应形成荧光基团的起始材料的常规策略,使用荧光吖啶酮衍生物作为原料,通过位置 - 取代基将该材料提供给反应性基团, 特异性亲电取代反应,然后使具有反应性基团的吖啶酮衍生物与氨基酸衍生物偶联。
    • 79. 发明授权
    • Chromogenic compounds, and use thereof as enzyme substrates
    • 显色化合物及其作为酶底物的用途
    • US07223865B2
    • 2007-05-29
    • US10541490
    • 2004-01-26
    • Arthur JamesAnnette Rigby
    • Arthur JamesAnnette Rigby
    • C07D219/00C12Q1/37
    • C12Q1/04C07D219/02C12Q1/37
    • The present invention relates to novel chromogenic substrates which are used to detect aminopeptidase activity in microorganisms or to determine whether at least one bacterium belongs to the Gram-positive group or to the Gram-negative group according to the color thereof. The invention also relates to culture media containing such substrates, to the use of the substrates or media for the detection of aminopeptidase activities and/or the differentiation of Gram-positive bacteria from Gram-negative bacteria and to methods of use.The aforementioned novel substrates have the formula below: in which: R1 is nothing or an alkyl, allyl or aryl group, R2 consists of at least one amino acid, preferably alanine, R3, R4, R5 and R6 consist, independently of one another, of H— or —O-alkyl, preferably —O—CH3, R7 consists of H, O—CH3, alkyl or halogen, R8 consists of H or Cl, and n is an integer corresponding to 0 or 1. The invention is particularly suitable for use in the field of diagnostics.
    • 本发明涉及用于检测微生物中氨基肽酶活性的新型显色底物,或根据其颜色确定至少一种细菌是否属于革兰氏阴性组或革兰氏阴性组。 本发明还涉及含有这种底物的培养基,使用底物或培养基来检测革兰氏阴性细菌中革兰氏阳性菌的氨基肽酶活性和/或分化以及使用方法。 上述新型底物具有下式:其中:R 1不是或烷基,烯丙基或芳基,R 2 2由至少一个氨基酸组成,优选 丙氨酸,R 3,R 4,R 5和R 6各自独立地为H - 或-O-烷基,优选-O-CH 3,R 7由H,O-CH 3,烷基或卤素组成, R 8由H或Cl组成,n是对应于0或1的整数。本发明特别适用于诊断领域。