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ID: ALA1143192
Journal: Bioorg Med Chem Lett
Title: Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists.
Authors: Ernst J, Dahl R, Lum C, Sebo L, Urban J, Miller SG, Lundström J.
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 (IC(50)<10nM) inhibitors of HIV-1 entry. One compound (40) was further profiled and was found to have attractive selectivity, pharmacokinetic, and antiviral properties.
CiteXplore: 18194864