Title of article
Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists
Author/Authors
Justin Ernst، نويسنده , , Russell Dahl، نويسنده , , Christopher Lum، نويسنده , , Lubomir Sebo، نويسنده , , Jan Urban، نويسنده , , Stephen G. Miller، نويسنده , , Jan Lundstr?m، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
1498
To page
1501
Abstract
A novel series of imidazopiperidine-tropane CCR5 antagonists is described. The series was optimized for anti-HIV-1 potency using a set of phenotypic viral entry assays. This strategy resulted in the identification of several very potent (IC50 < 10 nM) inhibitors of HIV-1 entry. One compound (40) was further profiled and was found to have attractive selectivity, pharmacokinetic, and antiviral properties.
Keywords
CCR5 , Chemokine receptor , CCR5 antagonist , HIV-1 entry , viral entry , Entry inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799194
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