CAS: 120013-56-1; 6-O-Desmethyl Donepezil

该化合物是Donepezil的化学化合物,主要用于治疗阿尔茨海默氏病,其特征是结构改变,特别是将甲状腺素组移走在Donepezil分子的6个位置上,结果,该物质可能表现出与其母体化合物不同的药理特性.通常,对6-O-demethy Donepezil等化合物的研究,研究其对乙酰胆碱酯酶抑制的潜在影响,这对加强脑胆碱性...

结构式图片

物理性质

MSDS等安全信息

上下游产品

donepezil 3-(4-hydroxy-3-methoxyphenyl)propionic acid 6-hydroxy-5-methoxyindan-1-one (E)-3-(4-hydroxy-3-methoxyphenyl)acrylic acid 1-benzyl-4-[(6-ethoxy-5-methoxy-1-indanon)-2-yl]methylpiperidine tert-butyl 2-(2-((1-benzylpiperidin-4-yl)methyl)-6-methoxy-3-oxo-2,3-dihydro-1H-inden-5-yloxy)acetate

合成工艺路线路线简述

    📜3-(4-羟基-3-甲氧基苯基)丙酸置于4-二甲氨基吡啶,甲烷磺酸,茴香硫醚,Palladium 10% On Activated Carbon,氢气,三乙胺,Potassium Hydroxide体系中,用 四氢呋喃,乙醇,二氯甲烷 用作溶剂,化学反应 2.08H,反应生成6-O-去甲基多奈哌齐
    参考文献:Multifunctional Donepezil Analogues As Cholinesterase And Bace1 Inhibitors
    标题:Multifunctional Donepezil Analogues As Cholinesterase And Bace1 Inhibitors
    摘要:一系列22个多奈哌齐类似物通过烷基化/苄基化合成,并与多奈哌齐及其6-去甲基加合物进行比较.发现所有化合物均是乙酰胆碱酯酶(ache)和丁酰胆碱酯酶(bche)的有效抑制剂,这两种酶在阿尔茨海默病患者大脑中负责水解神经递质乙酰胆碱.许多化合物的eeache(ic50 = 0.016 +/-0.001 µm至0.23 +/-0.03 µm)和efbche(ic50 = 0.11 +/-0.01 µm至1.3 +/-0.2 µm)的抑制浓度低于多奈哌齐.其中一种较好的化合物对hsache进行了测试,发现其比多奈哌齐更活跃,并且比eeache更好地抑制了hsache.具有芳香族取代基的类似物通常比具有脂肪族取代基的类似物更有效.其中五种类似物还抑制了β-分泌酶(bace1)酶的作用.
    Doi:10.3390/molecules23123252

    海关参考信息

    专利信息


    专利号:US-8580822-B2
    优先权日:2006-12-11
    标 题:Compositions, synthesis, and methods of using indanone based cholinesterase inhibitors
    发明人：BHAT LAXMINARAYAN; MOHAPATRA PRABHU PRASAD
    权利人:BHAT LAXMINARAYAN; MOHAPATRA PRABHU PRASAD; REVIVA PHARMACEUTICALS INC
    摘要:The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.

    专利号:US-2008153878-A1
    优先权日:2006-12-11
    标题:Compositions, synthesis, and methods of using indanone based cholinesterase inhibitors

    专利号:RU-2478619-C2
    优先权日:2006-12-11
    标 题:Compositions, synthesis and methods of using indanone based cholinesterase inhibitors

    专利号:JP-2010512328-A
    优先权日:2006-12-11
    标题:Composition, synthesis and method of use of indanone cholinesterase inhibitors

    专利号:CA-2672212-A1
    优先权日:2006-12-11
    标 题:Compositions, synthesis, and methods of using indanone based cholinesterase inhibitors

    专利号:US-8247563-B2
    优先权日:2006-12-11
    标题 :Compositions, synthesis, and methods of using indanone based cholinesterase inhibitors

    其他信息查阅

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    实用工具

    ⚠️全国化工行业净网倡议书
    📋制造商识别码
    📖 海关编码查询
    📝MSDS生成器

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    合成参考文献


    摘要:S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知