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Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists
Justin Ernst1, Russell Dahl, Christopher Lum
1Department of Medicinal Chemistry, Kémia, Inc., 5871 Oberlin Drive, San Diego, CA 92121, USA.
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.
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