Abstract
Incorporation of acidic functional groups into a lead CCR5 antagonist identified from a targeted combinatorial library resulted in compounds with enhanced anti-HIV-1 activity and attenuated L-type calcium channel affinity.
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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CHO Cells
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Calcium Channels, L-Type / drug effects
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Chemical Phenomena
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Chemistry, Physical
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Chemokine CCL4
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Cricetinae
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HIV-1 / drug effects*
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Half-Life
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HeLa Cells
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Humans
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Macrophage Inflammatory Proteins / antagonists & inhibitors
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Rats
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Receptors, CCR5 / chemistry
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Structure-Activity Relationship
Substances
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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Calcium Channels, L-Type
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Chemokine CCL4
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Macrophage Inflammatory Proteins
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Receptors, CCR5