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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters
