CAS: 59721-28-7; 4-(2-(2-(Dimethylamino)-2-Oxoethoxy)-2-Oxoethyl)Phenyl 4-Guanidinobenzoate

该化合物是一个合成精液蛋白抑制剂,主要以其在抑制酶转基因蛋白质2(TMPRSS2)的活动方面所起的作用而闻名.这种抑制作用在病毒感染方面意义重大,特别是在阻止包括冠状病毒在内的某些病毒进入宿主细胞方面.Camostat的特点是能够调节炎情反应,并且已经调查了各种条件下的潜在治疗用途,包括胰腺炎和纤维化.该化合物通常以盐盐的形式施用,这增加了其溶液性和生物利用率.Camostat表现出相对较低的毒性特征,使它成为了进一步研究抗病毒疗法的候选体.其行动机制涉及竞争性抑制,它与静液蛋白的活跃场所相连,从而防止亚质接触.

结构式图片

MSDS等安全信息

    上下游产品

    2-(二甲基氨基)-2-氧代乙基 2-(4-羟基苯基)乙酸酯 2-(Dimethylamino)-2-Oxoethyl 2-(4-Hydroxyphenyl)Acetate 59721-16-3

    合成工艺路线路线简述

      📜对胍基苯甲酸,2-(二甲基氨基)-2-氧代乙基 2-(4-羟基苯基)乙酸酯置于盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 乙腈 作为反应溶剂,化学反应 5.0H,以38.2 G的收率获得产物卡莫司他
      参考文献:一种酰基胍类化合物及其制备方法与应用
      标题:一种酰基胍类化合物及其制备方法与应用
      摘要:本发明公开了一种具有式i结构的酰基胍类化合物及其药学上可接受的盐.本发明还公开了上述化合物的制备方法,并同时公开了以该化合物或其药学上可接受的盐作为活性有效成分的药物组合物,以及他们在预防或治疗与精氨酸加压素v1A受体,精氨酸加压素v1B受体,精氨酸加压素v2受体相关的疾病(如高血压,慢性充血性心力衰竭,抗利尿激素分泌紊乱综合症或慢性心力衰竭/肝硬化/抗利尿激素分泌紊乱引起的低钠血症)中的应用.

      海关参考信息

      专利信息


      专利号:US-2025188022-A1
      优先权日:2022-02-07
      标 题 :Process for the preparation of nafamostat, camostat and their derivatives
      发明人:AHMED RIYAZ; KUMAR GULSHAN; MAHAJAN SHEENA; Verma Praveen Kumar; CHAM PANKAJ SINGH; KUMAR AMIT; AHMED QAZI NAVEED; REDDY DUMBALA SRINIVASA; SHANKAR RAVI; SINGH PARVINDER PAL
      权利人:COUNCIL SCIENT IND RES
      摘要:The invention provides a novel, economical and practical route for the synthesis of an ester from acid and alcoholic functionalities using Trihalotriazine as coupling agent. Specifically, the invention provides a novel, economical and practical route for the preparation of Nafamostat and Camostat. Synthesis of p-guanidinobenzoic acid (Al) was also achieved from thiourea and p-aminobenzoic acid by using trihalotriazine as coupling reagent.

      专利号:US-2024002405-A1
      优先权日:2022-06-01
      标题 :Antimicrobial compounds, synthesis methods, and uses thereof
      发明人:VERMA RAJNI; DONAVALLI KRISHNA MOHAN; ZAID GENE H
      权利人:ANKH LIFE SCIENCES LTD
      摘要:Fused tricyclic compounds and novel methods of synthesizing, using, and/or administering the same. Methods of inhibiting microbial activity and/or treating a microbial infection with fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds. The treatment of subjects suffering from a microbial infection comprises the step of administering to the subject one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds or a composition comprising one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds.

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      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: Hoffmann M, Hofmann-Winkler H, Smith JC, Krüger N, Sørensen LK, Søgaard OS, Hasselstrøm JB, Winkler M, Hempel T, Raich L, Olsson S, Yamazoe T, Yamatsuta K, Mizuno H, Ludwig S, Noé F, Sheltzer JM, Kjolby M, Pöhlmann S. Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity. bioRxiv [Preprint]. 2020 Aug
      5:2020.08.05.237651. doi: 10.1101/2020.08.05.237651.
      2: Bittmann S, Weissenstein A, Villalon G, Moschuring-Alieva E, Luchter E. Simultaneous Treatment of COVID-19 With Serine Protease Inhibitor Camostat and/or Cathepsin L Inhibitor? J Clin Med Res. 2020 May;12(5):320-322. doi: 10.14740/jocmr4161. Epub 2020 May 8.

      合成参考文献


      参考文献:10.1152/ajpgi.00426.2007
      摘要:Crozier SJ, Sans MD, Lang CH, D'Alecy LG, Ernst SA, Williams JA. CCK-induced pancreatic growth is not limited by mitogenic capacity in mice. American Journal of Physiology-Gastrointestinal and Liver Physiology. 2008 May;294(5):G1148–57. doi: 10.1152/ajpgi.00426.2007.
      参考文献:10.1021/acs.jmedchem.7b01698
      摘要:Pant SM, Mukonoweshuro A, Desai B, Ramjee MK, Selway CN, Tarver GJ, Wright AG, Birchall K, Chapman TM, Tervonen TA, Klefström J. Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform. J Med Chem. 2018 May 24;61(10):4335–47. doi: 10.1021/acs.jmedchem.7b01698.
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