Abstract
A combinatorial library of 28 pools of 180 compounds (345 diastereomers) was designed and prepared in support of the delineation of the SAR of two prototypical VLA-4 antagonists. Deconvolution of the active pools led to the identification of three novel series of VLA-4 antagonists with low nanomolar potencies.
MeSH terms
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / pharmacology
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Combinatorial Chemistry Techniques*
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Humans
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Inhibitory Concentration 50
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Integrin alpha4beta1 / antagonists & inhibitors*
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Jurkat Cells
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Molecular Mimicry
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Oligopeptides / chemical synthesis
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Oligopeptides / pharmacology
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents
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Integrin alpha4beta1
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Oligopeptides