Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors, Part 7. Synthesis, Antiviral Activity, and 3D-QSAR Investigations of Novel 6-(1-Naphthoyl) HEPT Analogues

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概要

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• A series of novel 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) analogues bearing a 6-(1-naphthoyl) group of non-nucleoside human immunodeficiency virus (HIV) reverse transcriptase inhibitors were synthesized and evaluated for their activity against HIV-1 and HIV-2. It was found that most of these compounds showed good activity against HIV-1. Among them, compound 5-isopropyl-6-(1-naphthoyl)-1-[(2E)-3-phenylallyl]-2, 4-pyrimidinedione (23) displayed the greatest inhibitory potency (IC_<50>=0.14μM), which is about 35-fold more active than HEPT and DDI. To rationalize the relationships between structure and activity of these novel compounds, a three-dimensional quantitative structure-activity relationship (3D-QSAR) model was also generated. The results provided a tool for guiding the further design of more potent antiviral agents and for predicting the affinity of related compounds.

• 公益社団法人日本薬学会の論文
• 2006-09-01

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

• CHEN Fen-Er

  Department of Chemistry, Fudan University

• Blanco Jose

  Departamento De Farmacologia Facultade De Farmacia Universidade De Santiago De Compostela

• Feng Xiao-qing

  Department Of Chemistry Fudan University

• 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

• 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

• Pannecouque Christophe

  Rega Inst. For Medical Res. Katholieke Universiteit Leuven

• JI Lei

  Department of Chemistry, Fudan University

• Ji Lei

  Department Of Chemistry Fudan University

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