CAS: 1111-39-3; 3'''-O-Acetyldigitoxin

该化合物是源自卡登酚的复杂胶层,其特点是卡登醇的类固基质特征,以其生物活动而著称,特别是在心脏胶层方面.多种糖浆的存在,特别是多头糖浆,特别是甲氧基-D-里博-赫索皮亚诺基元素,表明其具有大幅溶解和与生物系统互动的潜力.一个糖单位的消化表明其稳定性和生物利用率有所提高.卡登洛醇经常因其对心脏功能的影响而进行研究,而这种特殊化合物可能具有类似的药理特性.其结构复杂性意味着多种生物互动的潜力,使其成为医学化学和药理学的热点.

结构式图片

上下游产品

pyridine digitoxin 3',4'-di-O-acetyl digitoxin D-digitoxose Digitoxigenin digitoxin 3-dehydrodigoxigenin

合成工艺路线路线简述

    📜3"',4"'-Di-O-Acetyl Digitoxin置于水,Potassium Carbonate体系中,用 甲醇 用作溶剂,化学反应生成2-乙酰氨基-1,2,5-三脱氧-1,5-亚氨基-D-葡萄糖醇
    参考文献:Perfectly Regioselective Acylation Of A Cardiac Glycoside,Digitoxin,Via Catalytic Amplification Of The Intrinsic Reactivity
    标题:Perfectly Regioselective Acylation Of A Cardiac Glycoside,Digitoxin,Via Catalytic Amplification Of The Intrinsic Reactivity
    摘要:Organocatalytic Regioselective Acylation Of Digitoxin Has Been Developed. This Method Provides The 4'''-O-Manoacylate As The Sole Product Without The Concomitant Formation Of Diacylates. The Extremely High Regioselectivity Was Assumed To Be The Result From The Combined Effects Of The High Intrinsic Reactivity Of C(4''')-Oh And Catalyst-Promoted Regioselective Acylation Of The Same Hydroxy Group. (C) 2010 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Tetlet.2010.07.036

    海关参考信息

    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-10814013-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:US-6699676-B1
    优先权日:1999-06-03
    标题:Uses of ouabain and ouabain-like molecules in apoptosis related pathologies
    发明人:ORLOV SERGEI N; HAMET PAVEL; TREMBLAY JOHANNE
    权利人:CORP DU CT DE RECH DU CT HOSPI
    摘要:Longterm elevation of the intracellular Na + /K + ratio inhibits macromolecule synthesis and proliferation in the majority of cell types studied so far, including vascular smooth muscle cells (VSMC). We report here that inhibition of the Na + ,K + pump in VSMC by ouabain or 1 hour preincubation in K + -depleted medium attenuated apoptosis triggered by serum withdrawal, staurosporine or okadaic acid. In the absence of ouabain, both DNA degradation and caspase-3 activation in VSMC undergoing apoptosis were insensitive to modification of the extracellular Na + /K + ratio as well as to hyperosmotic cell shrinkage. In contrast, protection of VSMC from apoptosis by ouabain was abolished under equimolar substitution of Na + o with K + o , showing that the anti apoptotic action of Na + ,K + pump inhibition was caused by inversion of the intracellular Na + /K + ratio. Unlike VSMC, the same level of increment of the [Na + ] i /[K + ] i ratio caused by 2 hours preincubation of Jurkat cells with ouabain did not affect chromatin cleavage and caspase-3 activity triggered by treatment with Fas ligand, staurosporine or hyperosmotic shrinkage. Thus, our results show for the first time that similarly to cell proliferation, maintenance of a physiologically low intracellular Na + /K + ratio is required for progression of VSMC apoptosis.

    专利号:AU-2007308022-A2
    优先权日:2006-10-05
    标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:US-2008107598-A1
    优先权日:2006-10-05
    标 题:Efficient Synthesis of Chelators for Nuclear Imaging and Radiotherapy: Compositions and Applications

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Bodem G, Wirth K, Dengler HR. [Pharmacokinetic studies with alpha-acetyldigitoxin in man]. Verh Dtsch Ges Inn Med. 1974;80:1527-33. German. Spanish. German. Dutch. Review. Russian. Geriatrics. 1958 Feb;13(2):75-9. Spanish. French. Pharm Bull. 1957 Dec;5(6):627. French. German. German. Polish. Italian. French. Nord Med. 1958 Mar 6;59(10):351-3. Norwegian.

    合成参考文献


    摘要:Journal of Pharmacology and Experimental Therapeutics., 111(365), 1954 []
    参考文献:10.1021/jm0102811
    摘要:Farr CD, Tabet MR, Ball WJ, Fishwild DM, Wang X, Nair AC, Welsh WJ. Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis. J Med Chem. 2002 Jul 18;45(15):3257–70. doi: 10.1021/jm0102811.
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