CAS: 327036-89-5; Tdzd-8

该化合物是一种由五人环组成的含有硫磺和氮原子的环形环状的热循环化合物,该化合物具有硫氮和氮原子的衍生物,其核心为硫氮和亚氨酸酯,代之以苯基组和甲基组,有助于其独特的化学特性.二元功能组的存在表明,它具有两种碳基(C=O)功能,可以参与各种化学反应,包括核生殖添加和凝聚反应.分子结构表明,由于存在因其生物活动而闻名的硫氮和亚氨基胺框架,有可能在医药化学,特别是药品开发中应用.此外,该化合物可能会显示出令人感兴趣的物理特性,如有机溶剂中的溶解性以及受分子相互作用影响的具体熔点或沸点.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

N-benzyl-S-chloroisothi°Carbamoyl chloride Benzyl isothi°Cyanate methyl is°Cyanate

合成工艺路线路线简述

    📜N-Benzyl-S-Chloroisothiocarbamoyl Chloride 以 乙醇,正己烷 作为反应溶剂,化学反应 24.0H,反应生成 4-苄基-2-甲基-1,2,4-噻二唑烷-3,5-二酮
    参考文献:N-Benzylpiperidine Derivatives Of 1,2,4-Thiadiazolidinone As New Acetylcholinesterase Inhibitors
    标题:N-Benzylpiperidine Derivatives Of 1,2,4-Thiadiazolidinone As New Acetylcholinesterase Inhibitors
    摘要:A New Family Of 1,2,4-Thiadiazolidinone Derivatives Containing The N-Benzylpiperidine Fragment Has Been Synthesised. The Acetylcholinesterase (Ache) Inhibitory Activity Of All Compounds Was Measured Using Ellman'S Method And Some Of Them Turned Out To Be As Potent As Tacrine. Furthermore,Compound 13 Was As Active As Tacrine In Reversing The Blockade Induced By Tubocurarine At Rat Neuromuscular Junction. Additionally,Receptor Binding Studies Provided New Lead Compounds For Further Development Of Alpha (2)-Adrenergic And Sigma-Receptor Antagonists. Molecular Dynamic Simulation Using X-Ray Crystal Structure Of Ache From Torpedo Californica Was Used To Explain The Possible Binding Mode Of These New Compounds. (C) 2000 Editions Scientifiques Et Medicales Elsevier Sas.
    DOI:10.1016/s0223-5234(00)01166-1

    海关参考信息

    专利信息


    专利号:US-12410142-B2
    优先权日:2017-04-07
    标 题:Substituted imidazole salt compounds, preparation method thereof, pharmaceutical composition thereof and application thereof
    发明人:DENG XIANMING; LIN SHENGCAI; ZHANG CHENSONG
    权利人:XIAMEN VIVOHEALTHS TECH CO LTD
    摘要:Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals:

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    📌 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: Su C, Zhao N, Zou J, Yan X. TDZD-8 alleviates delayed neurological sequelae following acute carbon monoxide poisoning involving tau protein phosphorylation. Inhal Toxicol. 2020 Feb;32(2):79-85. doi: 10.1080/08958378.2020.1741739. Epub 2020 Mar 18. 23(5):405-415. doi: 10.1111/cns.12683. Epub 2017 Mar 2.
    3: Koehler D, Shah ZA, Williams FE. The GSK3β inhibitor, TDZD-8, rescues cognition in a zebrafish model of okadaic acid-induced Alzheimer's disease. Neurochem Int. 2019 Jan;122:31-37. doi: 10.1016/j.neuint.2018.10.022. Epub 2018 Oct 28.
    4: Liu Q, Kong Y, Guo X, Liang B, Xie H, Hu S, Han M, Zhao X, Feng P, Lyu Q, Dong W, Liang X, Wang W, Li C. GSK-3β inhibitor TDZD-8 prevents reduction of aquaporin-1 expression via activating autophagy under renal ischemia reperfusion injury. FASEB J. 2021 Aug;35(8):e21809. doi: 10.1096/fj.202100549R. 20(1):49. doi: 10.1186/s12974-023-02738-5.

    合成参考文献


    参考文献:10.1016/j.bmcl.2011.06.027
    摘要:Nasim S, Guzman ML, Jordan CT, Crooks PA. Discovery of 1,2,4-thiadiazolidine-3,5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture. Bioorganic & Medicinal Chemistry Letters. 2011 Aug;21(16):4879–83. doi: 10.1016/j.bmcl.2011.06.027.
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