CAS: 537-21-3; 1-(3,4-Dichlorophenyl)-5-Isopropylbiguanide

该化合物是一种属于大抗疟化合物的抗疟化合物,主要用于治疗和预防疟疾,特别是与其他抗疟剂结合使用;氯丙基甲醇的化学结构具有氯化联苯基和重氮酸盐的特性,有助于其药理活动;众所周知,氯丙基甲醇能够抑制疟疾寄生虫中的二氢氟酸还原酶酶酶,从而破坏顶部新陈代谢,并最终阻碍寄生虫的生长和繁殖;氯丙基甲醇通常通过口服方式施用,在水中具有中等溶解性,这可以影响其生物利用率;该化合物一般都经过良好调用,但与许多药物一样,可能会产生副作用,包括胃肠紊乱;当它与其他抗疟药物(如青蒿酸盐)结合使用时,其功效往往会提高,从而产生协同效应,减少抗药性发展的风险;

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    上下游产品

    3-cyano-1-isopropylguanidine 3,4-dichloroaniline hydr°Chloride N-cyano-N'-(3,4-dichloro-phenyl)-guanidineN-cyano-N'-(3,4-dichloro-phenyl)-guanidine isopropylamine hydr°Chloride2-[(3,4-dichlorophenyl)amino]-4-isopropylamino-[1,3,5]-triazine-6-carboxylic acid methyl ester 2-[(3,4-dichlorophenyl)amino]-4-isopropylamino-[1,3,5]-triazine-6-carboxylic acid benzyl ester N-(3,4-dichlorophenyl)-N'-isopropyl-6-phenyl-[1,3,5]-triazine-2,4-diamine 2-[(3,4-dichlorophenyl)amino]-4-isopropylamino-[1,3,5]-triazine-6-carboxylic acid ethyl ester

    合成工艺路线路线简述

      📜3,4-Dichloroaniline Hydrochloride置于水,硝基苯体系中,化学反应生成 氯丙胍
      参考文献:Crowther Et Al.,Journal Of The Chemical Society,1951,P. 1774,1778
      标题:Crowther Et Al.,Journal Of The Chemical Society,1951,P. 1774,1778

      海关参考信息

      专利信息


      专利号:US-9409879-B2
      优先权日:2011-03-29
      标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
      发明人：DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA
      权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT
      摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

      专利号:US-2014121238-A1
      优先权日:2011-03-29
      标 题:Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents

      专利号:WO-2012131010-A1
      优先权日:2011-03-29
      标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents

      专利号:CN-103534238-B
      优先权日:2011-03-29
      标题 :Total synthesis of redox-active 1.4‑naphthoquinone and its metabolites and their therapeutic use as antimalarial and schistosicides

      专利号:EP-2691372-A1
      优先权日:2011-03-29
      标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents

      专利号:EP-2691372-B1
      优先权日:2011-03-29
      标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents

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      主要参考文献


      1: Bukirwa H, Garner P, Critchley J. Chlorproguanil-dapsone for treating uncomplicated malaria. Cochrane Database Syst Rev. 2004 Oct 18;2004(4):CD004387. doi: 10.1002/14651858.CD004387.pub2.
      2: Noor N, Rattani A. Chlorproguanil-dapsone for malaria. Lancet. 2004 Nov 13-19;364(9447):1753-4. doi: 10.1016/S0140-6736(04)17390-X. 358(9289):1218-23. doi: 10.1016/S0140-6736(01)06344-9. Erratum in: Lancet 2001 Nov 3;358(9292):1556. 360(9340):1136-43. doi: 10.1016/s0140-6736(02)11198-6. 363(9424):1838-9. doi: 10.1016/S0140-6736(04)16390-3. 364(9447):1752-3; author reply 1753. doi: 10.1016/S0140-6736(04)17388-1. 41(10):2261-4. doi: 10.1128/AAC.41.10.2261.
      8: Elewa H, Wilby KJ. A Review of Pharmacogenetics of Antimalarials and Associated Clinical Implications. Eur J Drug Metab Pharmacokinet. 2017 Oct;42(5):745-756. doi: 10.1007/s13318-016-0399-1. 91(3):322-7. doi: 10.1016/s0035-9203(97)90093-6. 6(11):952-4. doi: 10.1046/j.1365-3156.2001.00751.x.

      合成参考文献


      参考文献:10.4269/ajtmh.2009.09-0351
      摘要:Tiono AB, Dicko A, Ndububa DA, Agbenyega T, Pitmang S, Awobusuyi J, Pamba A, Duparc S, Goh LE, Harrell E, Carter N, Ward SA, Greenwood B, Winstanley PA. Chlorproguanil-dapsone-artesunate versus chlorproguanil-dapsone: a randomized, double-blind, phase III trial in African children, adolescents, and adults with uncomplicated Plasmodium falciparum malaria. Am J Trop Med Hyg. 2009 Dec;81(6):969–78. doi: 10.4269/ajtmh.2009.09-0351.
      参考文献:10.2165/00003088-199223020-00005
      摘要:Murray M. P450 enzymes. Inhibition mechanisms, genetic regulation and effects of liver disease. Clin Pharmacokinet. 1992 Aug;23(2):132–46. doi: 10.2165/00003088-199223020-00005.
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