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

新一代非核苷类HIV逆转录酶抑制剂TMC125的研究进展 被引量：1

Progress in the New Generation Nonnucleoside Anti-HIV Reverse Transcriptase Inhibitors-TMC125
下载PDF
导出
摘要 阐述了新一代非核苷类逆转录酶抑制剂(Nonnucleosidereversetranscriptaseinhibitors,NNRTIs)TMC125的发现,抗艾滋病病毒、耐药菌株、I型人类免疫缺陷病毒(Humanimmunodeficiencyvirustype1,HIV-1)M亚型病毒以及和其它药物联合使用的活性,代谢稳定性的研究进展.TMC125除具有一般NNRTIs类药物所具有的优点外还有较高的对抗耐药菌株和HIV-1M亚型病毒活性,与其它药物联合使用成为现在治愈人类免疫缺陷病毒(Humanimmunodeficiencyvi-rus,HIV)新的希望. This article summarizes the development and the activity against human immunodeficiency virus type 1 （HIV-1）, nonnucleoside reverse transcriptase inhibitors （NNRTIs）-resistant viruses and HIV-1 group M subtypes of the new generation NNRTIs-TMC125 as well as its metabolic stability assays and the advantage of its combination with other NNRTIs. Besides the same advantage as other NNRTIs, TMC125 was highly active against mutants. It also showed some activity against a series of HIV-1 group M subtypes. Combining TMC125 with other NNRTIs is a potential route against acquired immunodeficiency syndrome （AIDS）.
作者 侯金明 黄山
机构地区 中国药科大学物理化学教研室
出处 《有机化学》 SCIE CAS CSCD 北大核心 2006年第12期1733-1738,共6页 Chinese Journal of Organic Chemistry
关键词 TMC125 非核苷类逆转录酶抑制剂 人类免疫缺陷病毒 艾滋病 TMC125 NNRTIs HIV AIDS
分类号 TQ464.8 [化学工程—制药化工]
  • 相关文献

参考文献19

  • 1De Clercq,E.Biochim.Biophys.Acta 2002,1587,258.
  • 2Deeks,S.G.J.Acquired Immune Defic.Syndr.2001,26,S25.
  • 3周婷,谢蓝.HIV非核苷类逆转录酶抑制剂研究进展[J].药学学报,2004,38(8):666-672. 被引量：17
  • 4Ludovici,D.W., Kukla,M.J., Grous,P.G., Krishnan,S.,Andries,K., Ren,J., de Bethune,M.P., Azijn,H., Pauwels,R., de Clercq,E., Arnold,E., Janssen,P.A.J.Bioorg.Med.Chem.Lett.2001,11,2225.
  • 5Ding,J., Das,K., Moereels,H., Koymans,L., Andries,K.,Cohen,J.Nat.Struct.Biol.1995,2,407.
  • 6Ludovici,D.W., Kavash,R.W., Kukla,M.J., Ho,C.Y., Ye,H., De Corte,B.L., Andries,K., de Bethune,M.-P., Azijn,H., Pauwels,R., Moereels,H.E.L., Heeres,J., Koymans,L.M.H., de Jonge,M.R., Van Aken,K.J.A., Daeyaert,F.F.D., Lewi,P.J., Das,K., Arnold,E., Janssen,P.A.J.Bioorg.Med.Chem.Lett.2001,11,2229.
  • 7Ludovici,D.W., De Corte,B.L., Kukla,M.J., Ye,H., Ho,C.Y., Lichtenstein,M.A., Kavash,R.W., Andries,K., de Bethune,M.-P., Azijn,H., Pauwels,R., Lewi,P.J., Heeres,J., Koymans,L.M.H., de Jonge,M.R., Van Aken,K.J.A.,Daeyaert,F.F.D., Das,K., Arnold,E., Janssen,P.A.J.Bioorg.Med.Chem.Lett.2001,11,2235.
  • 8Das,K., Clark,A.D.Jr., Lewi,P.J., Heeres,J., De Jonge,M.R., Koymans,L.M., Vinkers,H.M., Daeyaert,F., Ludovici,D.W., Kukla,M.J., De Corte,B., Kavash,R.W.,Ho,C.Y., Ye,H., Lichtenstein,M.A., Andries,K., Pauwels,R., De Bethune,M.-P., Boyer,P.L., Clark,P., Hughes,S.H., Janssen,P.A.J., Arnold,E.J.Med.Chem.2004,47,2550.
  • 9Carlo,F.P., Lewi,P.J., de Jonge,M., Daeyaert,F., Koymans,L., Vinkers,M., Michael,K., Jan,H.J.Computer-Aided Mol.Des.2003,17,129.
  • 10Tantillo,C., Ding,J., Jacobo-Molina,A., Janssen,P.A.,Arnold,E.J.Mol.Biol.1994,243.

二级参考文献30

  • 1Yu H, Kalyan D, Ding JP, et al. Structures of tyr188leu mutant and wild-type HIV-1 reverse transcriptase complexed with the non-nucleoside inhibitor HBY 097:inhibitor flexibility is a useful design feature for reducing drug resistance [J]. J Mol Biol, 199
  • 2Parreira RLT, Abrahao O, et al. Conformational preferences of non-nucleoside HIV-1 reverse transcriptase inhibitors [ J ]. Tetrahedron, 2001,57:3243 - 3253.
  • 3Barreca ML, Carotti A, Carrieri A, et al. Comparative molecular field analysis (CoMFA) and docking studies of non-nucleoside HIV-1 RT inhibitors (NNIs) [ J]. Bioorg Med Chem, 1999,7:2283 -2292.
  • 4Kalyan D, Ding JP, Yu H, et al. Crystal structures of 8-Cl and 9-Cl TIBO complexed with wild-type HIV-1 RT and 8-Cl TIBO complexed with the tyr181cys HIV-1 RT drug-resistant mutant [J]. J Mol Biol, 1996,264:1085- 1100.
  • 5Gonzales M J, Wu TD, Taylor J, et al. Extended spectrum of HIV-1 reverse transcriptase mutations in patients receiving multiple nucleoside analog inhibitors [J]. AIDS, 2003,17(6):791 -799.
  • 6Wang DP, Rizzo RC, Julian TR, et al. Antiviral drug desigh: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs [ J ].Bioorg Med Chem Lett, 2001,11:2799 -2802.
  • 7Ludovici DW, Kukla M J, Grous PG, et al. Evolution of anti-HIV drug candidates. part 1: from otanilinophenylacetamide (αt-APA) to imidoyl thiourea (ITU) [ J ]. Bioorg Med Chem Lett, 2001,11: 2225 -2228.
  • 8Ludovici DW, Kavash RW, Kukla M J, et al. Evolution of anti-HIV drug candidates. part 2: diaryltriazine (DATA) analogues [J]. Bioorg Med Chem Lett, 2001,11:2229 - 2234.
  • 9Hogberg M, Sahlberg B, Engelhardt P, et al. Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. synthesis and further structure-activity relationship studies of PETT analogues [ J ]. J Med Chem, 1999,42(20) :4150-4160.
  • 10Esnouf RM, Stuart DI, De Clercq E, et al. Models which explain the inhibition of reverse transcriptase by HIV-1-specific ( thio ) carboxanilide derivatives [ J ].Biochem Biophys Commun, 1997,234(2) :458 -464.

共引文献16

同被引文献78

引证文献1

二级引证文献11

有机化学
2006年 第12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