Reversible natural product glycosyltransferase-catalyzed reactions, compounds and related methods
    4.
    发明授权
    Reversible natural product glycosyltransferase-catalyzed reactions, compounds and related methods 有权
    可逆天然产物糖基转移酶催化反应,化合物及相关方法

    公开(公告)号:US09469864B2

    公开(公告)日:2016-10-18

    申请号:US14335067

    申请日:2014-07-18

    摘要: The present invention relates to methods of use of glycosyltransferases and related novel compounds. The invention exploits the reversibility of glycosyltransferases to generate new sugars, unnatural biomolecules and numerous one-pot reactions for generation of new biomolecules having varied backbones such as enediynes, vancomycins, bleomycins, anthracyclines, macrolides, pluramycins, aureolic acids, indolocarbazoles, aminglycosides, glycopeptides, polyenes, coumarins, benzoisochromanequinones, calicheamicins, erythromycin, avermectins, ivermectins, angucyclines, cardiac glycosides, steroids or flavinoids. In preferred embodiments, the invention specifically relates to biosynthesis of anticancer (the enediyne calicheamicin, CLM), anthelmintic agents (the macrolides avermectin, ivermectin and erythromycin) and antibiotic (the glycopeptide vancomycin, VCM) natural product-based drugs developed by reversible, bidirectional glycosyltransferase-catalyzed reactions.

    摘要翻译: 本发明涉及使用糖基转移酶和相关新化合物的方法。 本发明利用糖基转移酶的可逆性来产生新的糖,非天然生物分子和许多一锅反应,用于产生具有不同骨架的新的生物分子,所述新生物分子具有不同的骨架,例如恩二烯,万古霉素,博来霉素,蒽环类抗生素,大环内酯类,阿拉伯霉素,阿拉伯酸,吲哚糖苷, ,多烯,香豆素,苯并二叠氮醌,加利车霉素,红霉素,阿凡曼菌素,伊维来菌素,角叉菜苷,强心苷,类固醇或黄素类。 在优选的实施方案中,本发明特别涉及抗逆转(双胍),抗胆碱药物(大环内酯阿维菌素,伊维菌素和红霉素)和抗生素(甘氨酸万古霉素,VCM)基于天然产物的药物的生物合成 糖基转移酶催化反应。

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    10.
    发明申请
    4"-Deoxy-4"-(s)-amido avermectin derivatives 有权
    4“ - 脱氧-4” - (s) - 氨基阿维菌素衍生物

    公开(公告)号:US20050176656A1

    公开(公告)日:2005-08-11

    申请号:US10513247

    申请日:2003-05-06

    IPC分类号: C07H17/08 C07H19/01 A01N43/04

    CPC分类号: C07H19/01

    摘要: A compound of formula (I); that has the S-configuration at the 4″-position and wherein the bond between carbon atoms 22 and 23 is a single or a double bond; R1 is C1-C12alkyl, C3-C8cycloalkyl; or C2-C12alkenyl; R2 is H, or, for example, unsubstituted or mono- to penta-substituted C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl or C1-C6alkoxy-C1-C6alkyl; R3 is H or, for example, C1-C12alkyl; X is a bond, O, NR4 or S; and Z is C═O, C═S or S02; and, where applicable, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in salt form; a process for the preparation of and the use of those compounds and their isomers and tautomers; starting materials for the preparation of the compounds of formula (I); pesticidal compositions in which the active ingredient has been selected from those compounds and their tautomers; and a method of controlling pests using those compositions are described.

    摘要翻译: 式(I)化合物; 其在4“位具有S-构型,并且其中碳原子22和23之间的键是单键或双键; R 1是C 1 -C 12烷基,C 3 -C 8烷基,C 1 -C 12烷基,C 3 -C 12烷基, 环烷基 或C 2 -C 12 - 烯基; R 2是H,或者例如未取代的或一至五取代的C 1 -C 12烷基,C 1 -C 12烷基, C 1 -C 12烷基,C 2 -C 12炔基或C 1 -C 1烷基, C 1 -C 6烷氧基-C 1 -C 6烷基; R 3是H或例如C 1 -C 12烷基; X是键,O,NR 4或S; Z是C-O,C-S或S 0 <2个; 并且在适用的情况下,E / Z异构体,E / Z异构体和/或互变异构体的混合物,在每种情况下为游离形式或盐形式; 一种制备和使用这些化合物及其异构体和互变异构体的方法; 用于制备式(I)化合物的起始原料; 其中活性成分选自那些化合物及其互变异构体的杀虫组合物; 并描述了使用这些组合物来控制害虫的方法。