期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

富马酸替诺福韦酯合成路线图解 被引量：9

Graphical Synthetic Routes of Tenofovir Disoproxil Fumarate
下载PDF
导出
摘要 富马酸替诺福韦酯（teriofovir disoProxil fumarate，1），化学名为（R）-[[2-（6-氨基-9H-嘌呤-9-基）- 1-甲基乙氧基]甲基]膦酸二异丙氧羰氧基甲酯富马酸盐,是美国Gilead Sciences公司研发的核苷酸逆转录酶抑制剂，是替诺福韦（PMPA，2）的前药，2001年首次在美国上市，临床主要用于治疗人类免疫缺陷病毒（HIV）感染，
作者 顾飞军 刘燕刚
机构地区 上海交通大学药学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2008年第10期783-785,共3页 Chinese Journal of Pharmaceuticals
关键词 富马酸盐 合成路线图解 甲酯 人类免疫缺陷病毒 乙氧基 酶抑制剂 化学名 逆转录
分类号 TQ464.7 [化学工程—制药化工] TS202.3 [轻工技术与工程—食品科学]
  • 相关文献

参考文献16

  • 1Sorbera LA, Castaner J. (R) -PMPA and Bis (POC) PMPA [J]. Drugs Future, 1998, 23 (12): 1279-1286.
  • 2崔岚,安富荣,王晓珉.核苷酸逆转录酶抑制剂替诺福韦DF[J].中国新药杂志,2004,13(11):1054-1058. 被引量：30
  • 3龙亚秋.艾滋病治疗药物的研究进展[J].药学服务与研究,2007,7(6):401-407. 被引量：10
  • 4Quan DJ, Peters MG. Tenofovir disoproxil fumarate for the treatment of hepatitis B virus infection: pharmacokinetics and clinical efficacy [J]. Therapy, 2007, 4 (2) : 141-151.
  • 5Peters MG, Andersen J, Lynch P, et al. Randomized controlled study of tenofovir and adefovir in chronic hepatitis B virus and HIV infection: ACTG A5127 [J]. Hepatology, 2006, 44(5): 1110-1116.
  • 6杨兆新,房建山.无环核苷膦酸的前体药物:中国,1986553[P].2007-06-27.(CA2007,147:166578)
  • 7Holy A, Dvorakova H, Declercq EDA, et al. Antiretroviral enantiomeric nucleotide analogs: WO, 9403467 [P]. 1994-02-17. (CA 1995, 122: 106401)
  • 8Holy A, Masojidkova M. Synthesis of enantiomeric N- (2- phosphonomethoxypropyl) derivatives of purine and pyrimidine bases. Ⅰ. The stepwise approach [J]. Collect Czech Chem Commun, 1995, 60 (7) : 1196-1212.
  • 9Holy A, Dvorakova H, Masojidkova M. Synthesis of enantiomeric M- (2-phosphonomethoxypropyl) derivatives of purine and pyrimidine bases. Ⅱ. The synthon approach[J]. Collect Czech Chem Commun, 1995, 60 (8) : 1390-1409.
  • 10Arimilli MN, Cundy KC, Dougherty JP, et al. Nucleotide analogs: WO, 9804569 [J]. 1998-02-05. (CA 1998, 128: 140970)

二级参考文献34

  • 1[1]Robbins BL,Srinivas RV,Kim C,et al.Anti-human immunodeficiency virus activity and cellular metabolism of a potential prodrug of the acyclic nucleoside phosphonate 9-R-(2-phosphonomethoxypropyl)adenine (PMPA),Bis(isopropyloxymethylcarbonyl)PMPA[J].Antimicrob Agents Chemother,1998,42(3):612-617.
  • 2[2]Arimilli MN,Kim CU,Dougherty J,et al.Synthesis,in vitro biological evaluation and oral bioavailability of 9-[2-(phosphonomethoxy)propyl]adenine (PMPA) prodrugs[J].Antivir Chem Chemother,1997,8(6):557-564.
  • 3[3]Hossain MM,Coull JJ,Drusano GL,et al.Dose proportional inhibition of HIV-1 replication by mycophenolic acid and synergistic inhibition in combination with abacavir,didanosine,and tenofovir[J].Antiviral Res,2002,55(1):41-52.
  • 4[4]Cihlar T,Ho ES,Lin DC,et al.Human renal organic anion transporter 1 (hOAT1) and its role in the nephrotoxicity of antiviral nucleotide analogs[J].Nucleosides Nucleic Acids,2001,20(4-7):641-648.
  • 5[5]Zidek Z,Frankova D,Holy A.Activation by 9-(R)-[2-(phosphonomethoxy)propyl]adenine of chemokine (RANTES,macrophage inflammatory protein 1α) and cytokine (tumor necrosis factor α,interleukin-10[IL-10],IL-1β) production[J].Antimicrob Agents Chemother,2001,45(12):3381-3386.
  • 6[6]Van Gelder J,Deferme S,Annaert P,et al.Increased absorption of the antiviral ester prodrug tenofovir disoproxil in rat ileum by inhibiting its intestinal metabolism[J].Drug Metab Dispos,2000,28(12):1394-1396.
  • 7[7]Barditch-Crovo P,Deeks SG,Collier A,et al.Phase Ⅰ/Ⅱ trial of the pharmacokinetics,safety,and antiretroviral activity of tenofovir disoproxil fumarate in human immunodeficiency virus-infected adults[J].Antimicrob Agents Chemother,2001,45(10):2733-2739.
  • 8[8]Schooley RT,Ruane P,Myers RA,et al.Tenofovir DF in antiretroviral-experienced patients:results from a 48-week,randomized,double-blind study[J].AIDS,2002,16(9):1257-1263.
  • 9[9]Therese M,Chapman,Jane K,et al.Tenofovir disoproxil fumarate[J].Drugs,2003,63(15):1597-1608.
  • 10[10]Squires K,Pozniak AL,Pierone G Jr,et al.Tenofovir disoproxil fumarate in nucleoside-resistant HIV-1 infection:a randomized trial[J].Ann Intern Med,2003,139(5 Pt 1):313-320.

共引文献35

同被引文献96

引证文献9

二级引证文献28

中国医药工业杂志
2008年 第10期

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部