CAS: 7681-76-7; (1-Methyl-5-Nitro-1H-Imidazol-2-yl)Methyl Carbamate

该化合物是一种硝基甲基氮醇衍生物,具有很强的抗蛋白和抗菌特性,主要用于兽医治疗由厌氧细菌和原生动物(如家禽中的Hittomonas Meleagridis和鸽子中的Trichomonas物种)引起的感染,该化合物通过减少其硝基组破坏微生物DNA合成,导致细胞毒性效应.Ronidazole以其高效力,广谱活度和有利的药用植物特征而著称,确保有效的组织渗透;其稳定性和水中的低溶性适合口腔管理.适当的剂量对于尽量减少潜在抗药性和确保治疗成功至关重要.

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上下游产品

CAS号936-05-0 1-甲基-5-硝基-2-羟甲基咪唑

合成工艺路线路线简述

  • 合成目标产物 Ronidazole 主要起始原料 1-Methyl-5-Nitro-1H-Imidazole-2-Methanol
  • (文献来源)合成步骤主要原料 1-Methyl-5-Nitro-1H-Imidazole-2-Methanol
1-甲基-5-硝基-2-羟甲基咪唑置于ammonium Hydroxide,三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,反应生成 洛硝哒唑
参考文献:Discovery Of A Dual Tubulin Polymerization And Cell Division Cycle 20 Homologue Inhibitor Via Structural Modification On Apcin
标题:Discovery Of A Dual Tubulin Polymerization And Cell Division Cycle 20 Homologue Inhibitor Via Structural Modification On Apcin
摘要:Apcin Is One Of The Few Compounds That Have Been Previously Reported As A Cdc20 Specific Inhibitor,Although Cdc20 Is A Very Promising Drug Target. We Reported Here The Design,Synthesis,And Biological Evaluations Of 2,2,2-Trichloro-1-Aryl Carbamate Derivatives As Cdc20 Inhibitors. Among These Derivatives,Compound 9F Was Much More Efficient Than The Positive Compound Apcin In Inhibiting Cancer Cell Growth,But It Had Approximately The Same Binding Affinity With Apcin In Spr Assays. It Is Possible That Another Mechanism Of Action Might Exist. Further Evidence Demonstrated That Compound 9F Also Inhibited Tubulin Polymerization,Disorganized The Microtubule Network,And Blocked The Cell Cycle At The M Phase With Changes In The Expression Of Cyclins. Thus,It Induced Apoptosis Through The Activation Of Caspase-3 And Parp. In Addition,Compound 9F Inhibited Cell Migration And Invasion In A Concentration-Dependent Manner. These Results Provide Guidance For Developing The Current Series As Potential New Anticancer Therapeutics.
DOI:10.1021/acs.Jmedchem.9B02097

海关参考信息

专利信息


专利号:WO-2025086625-A1
优先权日:2023-10-26
标题 :Synthesis method for deuterated tinidazole
发明人:MEI SHU; GUO HUI; CHEN WULIAN
权利人:ANPEL LABORATORY TECH SHANGHAI INC
摘要:The present invention relates to a synthesis method for a deuterated tinidazole. The deuterated tinidazole is as represented by formula I, wherein one or more of R 1 -R 5 are deuterium, and the rest is hydrogen. The synthesis method comprises the step of oxidizing an intermediate B with m-chloroperoxybenzoic acid to prepare the deuterated tinidazole, wherein the oxidation is carried out under low-temperature and alkaline conditions; and the intermediate B is as represented by formula II. By using the synthesis method of the present invention, the problems of deuterium shedding and isotope dilution in the reaction process can be avoided, and the stable isotope-labeled deuterated tinidazole with the isotope abundance of > 98% is obtained with a higher yield. The prepared deuterated tinidazole can be used as an isotope internal standard reagent for the quantitative detection of tinidazole, which, for example, can be used to detect residual tinidazole in meat products by means of an isotope internal standard method, and has the advantages of having high recovery efficiency from a matrix, and being environmentally friendly and safe.

专利号:CN-117801027-A
优先权日:2023-07-03
标 题 :Synthesis of cobalt compound with spiral structure and application of cobalt compound in electrochemical detection

专利号:CN-107722288-B
优先权日:2017-10-18
标 题:Synthesis of a case of Eu-MOFs and its application in antibiotic identification

专利号:CN-108693152-B
优先权日:2018-03-06
标 题:Synthesis of tetranuclear copper-iodine cluster and antibiotic sensing application thereof

专利号:CN-107722288-A
优先权日:2017-10-18
标题 :Synthesis of a Eu‑MOFs material and its application in antibiotic identification

专利号:CN-108693152-A
优先权日:2018-03-06
标题 :Synthesis of a tetranuclear copper-iodide cluster and its application in antibiotic sensing
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主要参考文献


1: Jiang B, Liu Q, Wang M, Yang M, Li F, Zhang L, Zhou J. Development of purity certified reference materials to establish metrological traceability for the measurement of nitroimidazoles in agricultural products. Anal Bioanal Chem. 2024 Sep 19. doi: 10.1007/s00216-024-05530-3. Epub ahead of print. 89(11):7780-7789. doi: 10.1021/acs.joc.4c00448. Epub 2024 May 16.
2707:223-234. doi: 10.1007/978-1-0716-3401-1_15.
1702:464087. doi: 10.1016/j.chroma.2023.464087. Epub 2023 May 19. 20(3):95-102. doi: 10.1089/zeb.2022.0066. Epub 2023 May 25.

合成参考文献


摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
摘要:
参考文献:10.1016/0020-7519(80)90060-0
摘要:Jennings FW, Urquhart GM, Murray PK, Miller BM. ‘Berenil’ and nitroimidazole combinations in the treatment of Trypanosoma brucei infection with central nervous system involvement. International Journal for Parasitology. 1980 Feb;10(1):27–32. doi: 10.1016/0020-7519(80)90060-0.
参考文献:10.1007/bf03190008
摘要:Virkel G, Lifschitz A, Pis A, Lanusse C. Influence of diet on the pattern of gastrointestinal biotransformation of netobimin and albendazole sulphoxide in sheep. European Journal of Drug Metabolism and Pharmacokinetics. 1999 Mar;24(1):31–7. doi: 10.1007/bf03190008.
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