首页> 外国专利> NOVEL PHENOXAZINONE DERIVATIVES AS ENZYME SUBSTRATES AND USE THEREOF AS INDICATOR IN THE DETECTION OF MICROOGANISMS WITH PEPTIDASE ACTIVITY

NOVEL PHENOXAZINONE DERIVATIVES AS ENZYME SUBSTRATES AND USE THEREOF AS INDICATOR IN THE DETECTION OF MICROOGANISMS WITH PEPTIDASE ACTIVITY

机译:新型苯氧嗪酮衍生物作为酶基质,并以此为指示剂检测具有肽酶活性的微生物

摘要

pChromogenic enzyme substrates that are 7-amino-phenoxazine derivatives (I) are new. Chromogenic enzyme substrates that are 7-amino-phenoxazine derivatives of formula (I). R1 and R2 = hydrogen, 1-6C alkyl, halo, COOR', CONR'R'', sulfo, or sulfonamide, or together they complete a naphthalene ring or optionally substituted coumarin of formula (a); R3 and R4 = hydrogen, halo, COOR', CONR'R'', sulfo or sulfonamide, or together complete a naphthalene ring of formula (b); R5 and R6 = hydrogen, halo, COOR', CONR'R'' or 1-6C alkyl; R7 and R8 = hydrogen, 1-6C alkyl, aralkyl, aryl, carboxyalkyl, carboxy or sulfo, or together complete a 4-6C ring; R9 = hydrogen, bromo, chloro, benzoyl, carboxy or sulfo, but must be other than hydrogen if R5 is hydrogen; R' and R'' = hydrogen or 1-6C alkyl or together they complete a heterocycle containing one or more heteroatoms; A = at least one amino acid; X = blocking group or is absent; Provided that at least one of R1/R2 and R3/R4 forms a phenyl or optionally substituted coumarin ring, and when R1/R2 form a coumarin ring, then R3 and R4 do not form a phenyl ring; R6 is hydrogen when R1/R2 form a ring and is halo when R1/R2 and R3/R4 each form a benzene ring. Independent claims are also included for: (1) reaction medium that includes at least one (I), optionally also at least one other enzyme substrate (X) specific for an enzyme activity other than that detected by (I); (2) process for detecting, identifying and/or quantifying microorganisms that express at least one peptidase activity, using the medium of (1); (3) process for differentiating between Gram positive and negative bacteria, using a medium of (1) in which the (I) present includes an alanine residue; and (4) process for differentiating between Candida albicans and C. tropicalis or C. glabrata, using a medium of (1) in which the (I) present includes a proline residue./p [FR2854893A1]
机译:> 7-氨基-苯恶嗪衍生物(I)的发色酶底物是新的。发色酶底物是式(I)的7-氨基-苯恶嗪衍生物。 R1和R2 =氢,1-6C烷基,卤素,COOR′,CONR′R″,磺基或磺酰胺,或它们一起完成萘环或式(a)的任选取代的香豆素。 R3和R4 =氢,卤素,COOR′,CONR′R″,磺基或磺酰胺,或一起完成式(b)的萘环; R5和R6 =氢,卤素,COOR',CONR'R''或1-6C烷基; R7和R8 =氢,1-6C烷基,芳烷基,芳基,羧基烷基,羧基或磺基,或一起形成4-6C环; R9 =氢,溴,氯,苯甲酰基,羧基或磺基,但如果R5是氢,则必须不是氢。 R′和R″ =氢或1-6C烷基,或它们一起构成一个含有一个或多个杂原子的杂环。 A =至少一个氨基酸; X =阻止基团或不存在;只要R1 / R2和R3 / R4中至少一个形成苯基或任选取代的香豆素环,并且当R1 / R2形成香豆素环时,则R3和R4不形成苯环;当R1 / R2形成环时,R6是氢,当R1 / R2和R3 / R4各自形成苯环时,R6是卤素。还包括以下方面的独立权利要求:(1)反应介质,其包括除(I)所检测的酶活性以外的对酶活性具有特异性的至少一种(I),任选地还包括至少一种其他酶底物(X); (2)使用(1)的培养基检测,鉴定和/或定量表达至少一种肽酶活性的微生物的方法; (3)使用(1)的培养基区分革兰氏阳性菌和阴性菌的方法,其中存在的(I)包括丙氨酸残基; (4)使用(1)的培养基(其中存在的(I)包含脯氨酸残基)区分白色念珠菌和热带念珠菌或光滑念珠菌的方法。 [FR2854893A1]

著录项

  • 公开/公告号IN2005DN04817A

    专利类型

  • 公开/公告日2007-09-28

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN4817/DELNP/2005

  • 申请日2005-10-21

  • 分类号C07D265/36;

  • 国家 IN

  • 入库时间 2022-08-21 20:58:11

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