| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373070 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
Graphical abstractA 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
