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Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1 |
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| Authors: | Tallant Matthew D Duan Maosheng Freeman George A Ferris Robert G Edelstein Mark P Kazmierski Wieslaw M Wheelan Pat J |
| Affiliation: | a Department of Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA b Department of Virology, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA c ID DMPK, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA |
| Abstract: | We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model. |
| Keywords: | CCR5 HIV-1 Diaminobutane Tropane Benzimidazole |
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