CAS: 303-81-1; (3R,4S,5R,6R)-5-Hydroxy-6-((4-Hydroxy-3-(4-Hydroxy-3-(3-Methylbut-2-En-1-yl)Benzamido)-8-Methyl-2-Oxo-2H-Chromen-7-yl)Oxy)-3-Methoxy-2,2-Dimethyltetrahydro-2H-Pyran-4-Yl Carbamate

该化合物是一种氨基氨基甲胺抗生素,来源于Streptomyces niveus,主要以其针对细菌DNAgyras(二至一种乙异构体酶)的强效抑制性活动而闻名,具体针对具有ATP约束力的Gyras B子单元场地,使其对包括某些植物抗药性菌株在内的抗模性细菌有效;新生物素也展示了针对某些克格朗阴性生物的活动,并被研究其在抑制90(Hsp90)乳房细胞中热冲击蛋白的潜在作用,其独特的行动机制和选择性结合特性使其对研究应用,特别是微生物学和分子生物学研究具有价值,该化合物经常被用作抗生素抗药研究和细菌DNA复制研究的工具.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

CAS号1445875-24-0 (3R,4S,5R,6R)-6... | CAS号1476-53-5 新生霉素(钠盐) | CAS号4434-05-3 Notomycin A1

合成工艺路线路线简述

    📜(3R,4S,5R,6R)-6-((3-(4-((Tert-Butyldimethylsilyl)Oxy)-3-(3-Methylbut-2-En-1-yl)Benzamido)-4-Hydroxy-8-Methyl-2-Oxo-2H-Chromen-7-yl)Oxy)-5-Hydroxy-3-Methoxy-2,2-Dimethyltetrahydro-2H-Pyran-4-Yl Carbamate置于水,溶剂黄146,四甲基胍体系中,用 四氢呋喃,乙腈 用作溶剂,以58%的收率获得新生霉素
    参考文献:Chemoselective Enrichment For Compound Isolation
    标题:Chemoselective Enrichment For Compound Isolation
    摘要:通过形成聚合硅氧烷醚,可以实现对含有脂肪烃羟基和芳香族羟基化合物的化学选择性分离.本文描述了从聚合硅氧烷试剂中选择性释放含有脂肪烃羟基和芳香族羟基化合物的化学选择性.

    海关参考信息

    专利信息


    专利号:US-7230101-B1
    优先权日:2002-08-28
    标 题:Synthesis of methotrexate-containing heterodimeric molecules
    发明人:MURTHI KRISHNA K; SMITH CHASE C
    权利人:GPC BIOTECH INC
    摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

    专利号:WO-9943409-A1
    优先权日:1998-02-27
    标 题:Hplc fractionation of complex chemical mixtures
    发明人:COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN
    权利人:ISIS PHARMACEUTICALS INC; COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN
    摘要:The rapid deconvolution of complex chemical mixtures, such as combinatorial libraries prepared via solution-phase simultaneous addition of functionalities is demonstrated using HPLC. Libraries containing 25-216 members were screened for biological activity and active libraries are fractionated into discreet pools using preferred reversed-phase HPLC. The entire process can be completed from a single synthesis of 15-50 mg, without the need for fixed positions, serial synthesis, or tagging.

    专利号:US-5763625-A
    优先权日:1995-04-25
    标 题:Synthesis and use of β-lapachone analogs
    发明人:BOOTHMAN DAVID A; FRYDMAN BENJAMIN J; WITIAK DONALD T
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:3-Substituted-β-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-β-lapachones, 3-alkyl-β-lapachones and 3-halo-β-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.

    专利号:US-2025009786-A1
    优先权日:2021-09-30
    标 题 :Automated synthesis of polymeric dual drugs
    发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL
    权利人:SONY GROUP CORP
    摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.

    专利号:US-2022395555-A1
    优先权日:2020-06-11
    标题:Derivatives of antibiotics
    发明人:FARBER BORIS; FARBER SOF'YA; MARTYNOV ARTUR VIKTOROVICH
    权利人:FARBER BORIS; FARBER SOFYA; MARTYNOV ARTUR VIKTOROVICH
    摘要:Field of application: The invention relates to chemistry, pharmacy and cosmetology, allows to synthesize of supramolecular structure on base antibiotics derivatives for use in pharmacy, cosmetology and pharmacy. n The essence of the invention: a new derivatives of antibiotics based on supramolecular structures and a method for their preparation, characterized in that the supramolecular structures are obtained by combinatorial synthesis of an antibiotic from one source molecule with two or more groups available in the reaction for covalent modification, at least with two different modifiers simultaneously, this creates a mixture of modified derivatives of the original molecule, with a maximum variety of derivatives with forming new supramolecular structure, and as biologically active substances to create pharmaceutical compositions use such supramolecular structure without separation into individual components, and in the reaction a combinatorial mixture of modified derivatives of the original molecule is formed antibiotic, the maximum number of combinations. n Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.

    专利号:US-9890126-B2
    优先权日:2012-04-24
    标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF)
    发明人:HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W
    权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP
    摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 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: Dlugosz A, Janecka A. Novobiocin Analogs as Potential Anticancer Agents. Mini Rev Med Chem. 2017;17(9):728-733. doi: 10.2174/1389557516666161223155525. 140(22):6749-6753. doi: 10.1021/jacs.8b02283. Epub 2018 May 16.
    3: Riley HD Jr. Vancomycin and novobiocin. Med Clin North Am. 1970 Sep;54(5):1277-89. 50(9):1121-1127. doi: 10.1080/00498254.2019.1708514. Epub 2020 Jan 3.
    452:116-121. doi: 10.1016/j.carres.2017.10.011. Epub 2017 Oct 22. 139(48):17221-17224. doi: 10.1021/jacs.7b07736. Epub 2017 Nov 22.

    合成参考文献


    参考文献:10.1007/s00792-010-0303-x
    摘要:Romano I, Dipasquale L, Orlando P, Lama L, d'Ippolito G, Pascual J, Gambacorta A. Thermoanaerobacterium thermostercus sp. nov., a new anaerobic thermophilic hydrogen-producing bacterium from buffalo-dung. Extremophiles. 2010 Mar;14(2):233–40. doi: 10.1007/s00792-010-0303-x.
    参考文献:10.1016/j.jbiosc.2009.08.479
    摘要:Siebenberg S, Bapat PM, Lantz AE, Gust B, Heide L. Reducing the variability of antibiotic production in Streptomyces by cultivation in 24-square deepwell plates. Journal of Bioscience and Bioengineering. 2010 Mar;109(3):230–4. doi: 10.1016/j.jbiosc.2009.08.479.
    参考文献:10.1007/978-1-61779-182-6_11
    摘要:Banfalvi G. Synchronization of Bacillus subtilis cells by spore germination and outgrowth. Methods Mol Biol. 2011;761():163–71. doi: 10.1007/978-1-61779-182-6_11.
    参考文献:10.1021/ci2002236
    摘要:Huang XY, Shan ZJ, Zhai HL, Li LN, Zhang XY. Molecular design of anticancer drug leads based on three-dimensional quantitative structure-activity relationship. J Chem Inf Model. 2011 Aug 22;51(8):1999–2006. doi: 10.1021/ci2002236.
    参考文献:10.1007/s00203-011-0730-9
    摘要:Chen WM, Sheu FS, Sheu SY. Aquimarina salinaria sp. nov., a novel algicidal bacterium isolated from a saltpan. Arch Microbiol. 2012 Feb;194(2):103–12. doi: 10.1007/s00203-011-0730-9.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知