Abstract
The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacokinetics.
MeSH terms
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Animals
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / pharmacokinetics
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Anti-HIV Agents / pharmacology
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CCR5 Receptor Antagonists*
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Dogs
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Half-Life
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Humans
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Leukocytes, Mononuclear
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Macaca mulatta
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Metabolic Clearance Rate
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Piperidines / chemistry
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Pyrrolidines / chemical synthesis
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Pyrrolidines / pharmacokinetics*
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Pyrrolidines / pharmacology
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Radioligand Assay
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Rats
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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Piperidines
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Pyrrolidines
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piperidine