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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

DOI: 10.1016/j.bmcl.2007.12.058