CAS: 72744-67-3; (5Ar,10Ar)-5A,6,8,10A-Tetrahydro-1H-Dithiazolo[3,2-B:4',2'-E]Pyra Zine-3,5,10-Trione

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    CAS号34592-47-7 L-硫代脯氨酸 | CAS号67089-84-3 (R)-thiazolidin... | CAS号60664-15-5 ethyl L-thiazol...

    合成工艺路线路线简述

    • 合成目标产物 5,11-Bisthio-(R,R)-1,7-Diazatricyclo[7.3.0.07,11]Dodecane-2,8-Diketone 主要起始原料 4-Thiazolidinecarboxylic Acid, Hydrochloride (1:1), (4R)-
    • (文献来源)合成步骤主要原料 4-Thiazolidinecarboxylic Acid, Hydrochloride (1:1), (4R)-
    N-BOC-(R)-噻唑-4-羧酸 在 4-二甲氨基吡啶,1-羟基苯并三唑,N,N-二异丙基乙胺,N,N'-二异丙基碳二亚胺,三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺作为反应溶剂,反应 3.5H,获得 (5Ar,10Ar)-Tetrahydro-3H,5H,8H,10H-Bisthiazolo<3,4-A:3',4'-D>Pyrazine-5,10-Dione
    参考文献:Anti-Biofilm And Anti-Adherence Properties Of Novel Cyclic Dipeptides Against Oral Pathogens
    标题:Anti-Biofilm And Anti-Adherence Properties Of Novel Cyclic Dipeptides Against Oral Pathogens
    摘要:Microorganisms Embedded In A Biofilm Are Significantly More Resistant To Antimicrobial Agents And The Defences Of The Human Immune System,Than Their Planktonic Counterpart. Consequently,Compounds That Can Inhibit Biofilm Formation Are Of Great Interest For Novel Therapeutics. In This Study,A Screening Approach Was Used To Identify Novel Cyclic Dipeptides That Have Anti-Biofilm Activity Against Oral Pathogens. Five New Active Compounds Were Identified That Prevent Biofilm Formation By The Cariogenic Bacterium Streptoocus Mutans And The Pathogenic Fungus Candida Albicans. These Compounds Also Inhibit The Adherence Of Microorganisms To A Hydroxylapatite Surface. Further Investigations Were Conducted On These Compounds To Establish The Structure-Activity Relationship,And It Was Deduced That The Common Cleft Pattern Is Required For These Molecules To Act Effectively Against Biofilms.
    Doi:10.1016/J.Bmc.2018.11.042

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    参考文献:10.1016/j.bmc.2018.11.042
    摘要:Simon G, Bérubé C, Voyer N, Grenier D. Anti-biofilm and anti-adherence properties of novel cyclic dipeptides against oral pathogens. Bioorg Med Chem. 2019 Jun 15;27(12):2323–31. doi: 10.1016/j.bmc.2018.11.042.
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