Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists |
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| Authors: | Ernst Justin Dahl Russell Lum Christopher Sebo Lubomir Urban Jan Miller Stephen G Lundström Jan |
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| Affiliation: | Department of Medicinal Chemistry, Kémia, Inc., 5871 Oberlin Drive, San Diego, CA 92121, USA. |
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| 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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