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    METHOD OF DETERMINING THE ACTIVITY OF ENZYMES CONVERTING CYTOSINE DERIVATIVES TO URACIL DERIVATIVES IN CELLS, TISSUES AND ORGANISMS
    69.
    发明公开
    METHOD OF DETERMINING THE ACTIVITY OF ENZYMES CONVERTING CYTOSINE DERIVATIVES TO URACIL DERIVATIVES IN CELLS, TISSUES AND ORGANISMS 审中-公开
    测定胞嘧啶衍生物在细胞，组织和器官中转化为胞嘧啶衍生物的酶活性的方法

    公开(公告)号：EP3186387A1

    公开(公告)日：2017-07-05

    申请号：EP15774495.4

    申请日：2015-08-25

    申请人： Univerzita Palackého v Olomouci ,  Ustav organicke chemie a biochemie AV CR, v.v.i. ,  Institute of Applied Biotechnologies, A.S.

    发明人： KOBERNA, Karel ,  LIGASOVA, Anna ,  ROSENBERG, Ivan ,  LIBOSKA, Radek ,  PAV, Ondrej ,  KVAPIL, Petr ,  FISER, Josef

    IPC分类号： C12Q1/34

    CPC分类号： C12Q1/34 ,  G01N2333/978

    摘要： The invention provides a method of determining the deaminase activity of the enzymes transforming cytosine derivatives into uracil derivatives in a sample, wherein the sample is incubated with a substrate of an enzyme selected from a group comprising 5-ethynyl-2'- deoxycytidine (EdC), 5-bromo-2'-deoxycytidine (BrdC), 5-chloro-2'-deoxycytidine (CldC), 5-iodo-2'-deoxycytidine (IdC), 5-ethynylcytidine (EC), 5-bromocytidine (BrC), 5- chlorocytidine (CIC), 5-iodocytidine (IC) and 5-fluorocytidine (FC), whereas the substrates in the presence of enzymes transforming cytosine derivatives into uracil derivatives are subsequently transformed in the sample into deaminated products, EdC is transformed into 5-ethynyl-2'-deoxyuridine (EdU), BrdC into 5-bromo-2'-deoxyuridine (BrdU), CldC into 5-chloro-2'-deoxyuridine (CldU), IdC into 5-iodo-2'-deoxyuridine (IdU), EC into 5- ethynyluridine (EU), BrC into 5-bromouridine (BrU), CIC into 5-chlorouridine (CIU), IC into 5-iodouridine (IU) and FC into 5-fluorouridine (FU), these deaminated products are subsequently detected in the DNA or RNA and the amount of incorporated EdU, BrdU, CldU, or IdU in the DNA, and EU, BrU, CIU, IU, or FU in the RNA are determined. The invention also includes the use of the above-mentioned method for determining the deaminase activity in cells treated with substances, which influence the deaminase activity of the enzymes transforming cytosine derivatives into uracil derivatives.

    摘要翻译： 本发明提供测定样品中将胞嘧啶衍生物转化为尿嘧啶衍生物的酶的脱氨酶活性的方法，其中所述样品与选自5-乙炔基-2'-脱氧胞苷（EdC） ，5-溴-2'-脱氧胞苷（BrdC），5-氯-2'-脱氧胞苷（CldC），5-碘-2'-脱氧胞苷（IdC），5-乙炔基胞苷（EC），5-溴胞苷（BrC） ，5-氯胞苷（CIC），5-碘胞苷（IC）和5-氟胞苷（FC），然后在酶的存在下将底物转化为尿嘧啶衍生物，随后将样品转化成脱氨基产物，将EdC转化成 （EdU），BrdC转化为5-溴-2'-脱氧尿苷（BrdU），将CldC转化为5-氯-2'-脱氧尿苷（CldU），将IdC转化为5-碘-2'-脱氧尿苷 （IU），EC转化为5-乙炔基尿苷（EU），将BrC转化为5-溴尿苷（BrU），将CIC转化为5-氯尿苷（CIU），将IC转化为5-碘尿苷（IU） （FU），随后在DNA或RNA中检测这些脱氨基产物，并测定RNA中DNA和EU，BrU，CIU，IU或FU中掺入的EdU，BrdU，CldU或IdU的量。 本发明还包括使用上述方法测定用物质处理的细胞中的脱氨酶活性，所述物质影响将胞嘧啶衍生物转化为尿嘧啶衍生物的酶的脱氨酶活性。

    Lipophosphonoxins, method of their preparation and use
    70.
    发明公开
    Lipophosphonoxins, method of their preparation and use 有权
    Lipophosphonoxine，Verfahren zur Herstellung und Verwendung

    公开(公告)号：EP2527351A1

    公开(公告)日：2012-11-28

    申请号：EP12169491.3

    申请日：2012-05-25

    申请人： Ustav Organicke Chemie A Biochemie Av Cr, V.v.i. ,  Mikrobiologicky Ustav AV CR V.V.I. ,  Ustav Molekularni Genetiky Av Cr, V.v.i. ,  Trios, spol. s r.o.

    发明人： Rejman, Dominik ,  Pohl, Radek ,  Bartunek, Petr ,  Ribeiro Pombinho, Antonio Jose ,  Krasny, Libor ,  Latal, Tomas

    IPC分类号： C07F9/6558 ,  C07F9/6561 ,  A61K31/675 ,  A61P31/04

    CPC分类号： C07F9/6561 ,  C07F9/65586

    摘要： The invention discloses lipophosphonoxins of general formula I, wherein R 1 is (C 8 -C 22 )alkyl or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl and R 2 is uracil, thymin or cytosin, R 3 is selected from group comprising compounds of general formula II and III, where R 4 is H or CH 2 OH, R 5 is H or OH, R 6 is H or OH, R 7 is H or CH 2 OH, R 8 is H or CH 2 OH, R 9 is H or OH, R 10 is H or OH, R 11 is H or OH, R 12 is H or CH 2 OH. Described are also diastereomers and mixtures of diastereomers of compounds of general formula I as well as corresponding pharmaceutically acceptable salts and hydrates and also a suitable method of preparation of such compounds. All described compounds of general formula I can be used as antibacterial agents or as active components of disinfectants and/or of selective in vitro growth media.

    摘要翻译： 本发明公开了通式Ⅰ的脂磷氧化还原剂，其中R 1为（C 8 -C 22）烷基或十六烷氧基丙基，十四烷氧基丙基，十四烷氧基乙基或十六烷氧基乙基，R 2为尿嘧啶，甲氨宁或细胞碱，R 3选自通式 II和III，其中R 4是H或CH 2 OH，R 5是H或OH，R 6是H或OH，R 7是H或CH 2 OH，R 8是H或CH 2 OH，R 9是H 或OH，R 10为H或OH，R 11为H或OH，R 12为H或CH 2 OH。 还描述了通式I化合物的非对映异构体和非对映异构体的混合物，以及相应的药学上可接受的盐和水合物，以及这些化合物的合适的制备方法。 所有描述的通式I化合物可用作抗菌剂或作为消毒剂和/或选择性体外生长培养基的活性成分。