CAS: 1750-45-4; 5-Chloro-6-Hydroxybenzo[d]Oxazol-2(3H)-One

结构式图片

相似化合物

19932-84-4 1784060-40-7 78213-03-3

欧盟法规

ECHA物质C&L通报

上下游产品

5-chloro-2-benzoxazolinone buprenorphine hydr°Chloride

合成工艺路线路线简述

  • 3520-14-7 + 483-14-7 = 1750-45-4 + 153212-75-0 + 5719-85-7 + 62-99-7 + 125-73-5 + 92340-57-3 + 93-35-6 + 103-90-2
    反应条件:1.1 Catalysts: Nadph,Nadp,Magnesium Chloride,Cytochrome P450 Cyp1A2 Solvents: Dimethyl Sulfoxide,Water; Ph 7.4,37 °C
    标题:Stereoselective Interaction Between Tetrahydropalmatine Enantiomers And Cyp Enzymes In Human Liver Microsomes
    作者:Sun,Si-Yuan; Wang,Yu-Qing; Li,Li-Ping; Wang,Lu; Zeng,Su; Et Al
    参考文献:Chirality 日期:2013 卷标:25(1) 页码:43-47
📜氯唑沙宗置于glucose Dehydrogenase,葡萄糖,Cyp102A7 A266G,还原型辅酶ii(Nadph)四钠盐,Sodium Hydroxide体系中,用 二甲基亚砜 用作溶剂,化学反应 14.0H,以12%的收率获得6-.羟基氯唑沙宗
参考文献:用于细菌代谢产物合成的细菌和真菌双功能细胞色素p450酶的多样化文库
标题:用于细菌代谢产物合成的细菌和真菌双功能细胞色素p450酶的多样化文库
摘要:从零开始开发了用于制备药物代谢物的创新性生物羟基化催化剂.通过蛋白质序列比对鉴定了一组推定的和已知的双功能p450酶的细菌和真菌序列,该序列在大肠杆菌中表达并进行了表征.值得注意的是,来自烟曲霉的真菌自足细胞色素p450(cyp)结果证明在催化剂的制备和应用期间以及在有机助溶剂的存在下,该化合物特别稳定.为了提高具有高表达水平的那些变体的催化活性并拓宽底物特异性,引入了突出的单个突变.然后将选定的改良变体用作冻干细菌裂解物,用于合成4'-羟基双氯芬酸和6-羟基氯唑沙宗,活性药物化合物双氯芬酸和氯唑沙宗的两种代谢物代表与人p450产生的相同的代谢物.
Doi:10.1002/adsc.200900190

海关参考信息

专利信息


专利号:US-2021062179-A1
优先权日:2015-02-26
标题 :Microsomal bioreactor for synthesis of drug metabolites
发明人:KRISHNAN SADAGOPAN; WALGAMA CHARUKSHA THAMEERA; NERIMETLA RAJASEKHARA REDDY
权利人:UNIV OKLAHOMA STATE
摘要:Reusable microsomal biocatalytic systems (bioreactors) constructed on carbon nanostructure modified electrodes are provided. The bioreactors comprise stable, biologically active immobilized enzymes such as human cytochromes P 450 (CYPs) and their redox partner proteins, e.g. CYP-NADPH (reduced nicotinamide adenine dinucleotide phosphate) reductases (CPR), on the carbon nanostructure surface. The immobilized enzymes may be present in liver microsomes, such as human liver microsomes (HLM) or as bactosomes, S9 fractions, etc. The bioreactors are used, for example, for synthesizing metabolites of interest from compounds such as drugs that are catabolized by the enzymes.

专利号:US-2018044657-A1
优先权日:2015-02-26
标 题 :Microsomal bioreactor for synthesis of drug metabolites

专利号:WO-2016138477-A1
优先权日:2015-02-26
标题:Microsomal bioreactor for synthesis of drug metabolites

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

[参考文献]: Astrid Jordet Langhammer, Et Al. Fennel And Raspberry Leaf As Possible Inhibitors Of Acetaminophen Oxidation. Phytother Res. 2014 Oct;28(10):1573-6.
[参考文献]: Dany Spaggiari, Et Al. Comparison Of Liquid Chromatography And Supercritical Fluid Chromatography Coupled To Compact Single Quadrupole Mass Spectrometer For Targeted In Vitro Metabolism Assay. J Chromatogr A. 2014 Dec 5:1371:244-56.
[参考文献]: Hsien-Tsung Yao, Et Al. Effect Of Commercially Available Green And Black Tea Beverages On Drug-Metabolizing Enzymes And Oxidative Stress In Wistar Rats. Food Chem Toxicol. 2014 Aug:70:120-7.
[参考文献]: Jang Su Jeon, Et Al. Metabolic Characterization Of Meso-Dihydroguaiaretic Acid In Liver Microsomes And In Mice. Food Chem Toxicol. 2015 Feb:76:94-102.
[参考文献]: Julia Dinger, Et Al. Development Of An In Vitro Cytochrome P450 Cocktail Inhibition Assay For Assessing The Inhibition Risk Of Drugs Of Abuse. Toxicol Lett. 2014 Oct 1;230(1):28-35.

合成参考文献


参考文献:10.1191/096032701680350587
摘要:Loizou GD, Cocker J. The effects of alcohol and diallyl sulphide on CYP2E1 activity in humans: a phenotyping study using chlorzoxazone. Hum Exp Toxicol. 2001 Jul;20(7):321–7. doi: 10.1191/096032701680350587.
参考文献:10.1124/dmd.32.6.647
摘要:Walsky RL, Obach RS. Validated assays for human cytochrome P450 activities. Drug Metab Dispos. 2004 Jun;32(6):647–60. doi: 10.1124/dmd.32.6.647.
参考文献:10.1124/dmd.107.017442
摘要:Ahn CY, Bae SK, Jung YS, Lee I, Kim YC, Lee MG, Shin WG. Pharmacokinetic parameters of chlorzoxazone and its main metabolite, 6-hydroxychlorzoxazone, after intravenous and oral administration of chlorzoxazone to liver cirrhotic rats with diabetes mellitus. Drug Metab Dispos. 2008 Jul;36(7):1233–41. doi: 10.1124/dmd.107.017442.
参考文献:10.1111/bph.14776
摘要:Trousil S, Lee P, Edwards RJ, Maslen L, Lozan‐Kuehne JP, Ramaswami R, Aboagye EO, Clarke S, Liddle C, Sharma R. Altered cytochrome 2E1 and 3A P450‐dependent drug metabolism in advanced ovarian cancer correlates to tumour‐associated inflammation. British J Pharmacology. 2019 Aug 05;176(18):3712–22. doi: 10.1111/bph.14776.
参考文献:10.1016/j.lfs.2006.07.016
摘要:Kim YC, Lee I, Kim SG, Ko SH, Lee MG, Kim SH. Effects of glucose supplementation on the pharmacokinetics of intravenous chlorzoxazone in rats with water deprivation for 72 h. Life Sci. 2006 Nov 02;79(23):2179–86. doi: 10.1016/j.lfs.2006.07.016.
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