Abstract
Spirodiketopiperazine-based CCR5 antagonists, showing improved pharmacokinetic profiles without reduction in antagonist activity, were designed and synthesized. We also demonstrate the anti-HIV activity of a representative compound 12, as measured in a p24 assay.
Copyright 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacokinetics*
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CCR5 Receptor Antagonists*
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HIV Core Protein p24 / metabolism
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Humans
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Microsomes, Liver / metabolism
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Piperazines / chemical synthesis
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Piperazines / chemistry
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Piperazines / pharmacokinetics*
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Rats
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Receptors, CCR5 / metabolism
Substances
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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HIV Core Protein p24
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Piperazines
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Receptors, CCR5