Abstract
Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from beta-substituted (2R,3R)-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of MIP-1alpha to human CCR5, compared with the non-hydroxylated derivatives and the other isomers.
MeSH terms
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Animals
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Anti-HIV Agents / chemical synthesis*
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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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Chemokine CCL3
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Chemokine CCL4
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Chromatography, High Pressure Liquid
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Combinatorial Chemistry Techniques
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Cricetinae
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Cricetulus
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Drug Design
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Humans
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Hydroxylation
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In Vitro Techniques
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Indicators and Reagents
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Isomerism
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Macrophage Inflammatory Proteins / metabolism
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Magnetic Resonance Spectroscopy
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Microsomes, Liver / enzymology
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Microsomes, Liver / metabolism
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Oxidation-Reduction
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Protein Binding
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Rats
Substances
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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Chemokine CCL3
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Chemokine CCL4
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Indicators and Reagents
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Macrophage Inflammatory Proteins