Nonnucleoside HIV-1 Reverse-Transcriptase Inhibitors, Part 5. : Synthesis and Anti-HIV-1 Activity of Novel 6-Naphthylthio HEPT Analogues

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概要

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• As part of a series of studies to discover new HIV reverse-transcriptase inhibitors, various novel 6α- and 6β-naphthylthio 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio) thymine (HEPT) derivatives were synthesized, and in vitro anti-HIV-1 activity was evaluated. The results revealed that most of 6α-naphthylthio HEPT derivatives (7a-w) showed good activity [for 7e, IC_<50> value of 0.048μm and selectivity index (SI) value of 735; for 7h, IC_<50> value of 0.057μm and SI value of 579; for 7k, IC_<50> value of 0.063μm and SI value of 565], 6β-naphthylthio HEPT derivatives (8a-f) showed low activity, but the introduction of α nitro group to the C-1 position of the 6β-naphthyl ring in the 6β-naphthylthio series (11a-c) resulted in a dramatic increase in anti-HIV-1 activity.

• 公益社団法人日本薬学会の論文
• 2005-08-01

著者

• BALZARINI Jan

  Rega Institute for Medical Research, Katholieke Universiteit Leuven

• PANNECOUQUE Christophe

  Rega Institute for Medical Research, Katholieke Universiteit Leuven

• CLERCQ Erik

  Rega Institute for Medical Research, Katholieke Universiteit Leuven

• Wang Yue

  Department Of Computer Science University Of Tokyo

• Blanco Jose

  Departamento De Farmacologia Facultade De Farmacia Universidade De Santiago De Compostela

• Clercq Erik

  Rega Instituut Katholieke Universiteit Leuven

• Clercq Erik

  Rega Institute For Medical Research Katholieke Universiteit Leuven

• Balzarini J

  Rega Inst. For Medical Res.

• Chen Fen-er

  Dep. Of Chemistry Fudan Univ.

• Chen Fen-er

  Department Of Chemistry Fudan University

• Chen Fen

  Department Of Chemistry Fudan University

• Pannecouque Christophe

  Rega Instituut Katholieke Universiteit Leuven

• Pannecouque C

  Katholieke Univ. Leuven Leuven Bel

• Balzarini Jan

  Rega Inst. For Medical Res.

• Balzarini J

  Rega Institute For Medical Research Katholieke Universiteit Leuven

• Chen Xu

  School Of Pharmaceutical Engineering Shenyang Pharmaceutical University

• Pannecouque Christophe

  Rega Inst. For Medical Res. Katholieke Universiteit Leuven

• Chen Xu-xiang

  Fudan-dsm Joint Lab. For Synthetic Method And Chiral Technol. Dep. Of Chemistry Fudan Univ.

• Sun Guang

  Department of Obstetrics and Gynecology, Hamamatsu University School of Medicine

• Sun Guang

  Department Of Chemistry Fudan University

• Wang Yue

  Department Of Applied Chemistry Beijing Institute Of Petrochemical Technology

• Sun Guang-Fu

  Department of Chemistry, Fudan University

• Chen Xu-Xiang

  School of Pharmaceutical Engineering, Shenyang Pharmaceutical University

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