Abstract
We describe a novel series of imidazopyridine substituted phenylalanines which are potent VLA-4 antagonists. A wide variety of substituents are tolerated as replacements for the pendant 3-pyridyl ring. A clear structure-activity relationship was identified around the substitution of the 3-amino-cyclobut-2-enone portion of the molecule.
MeSH terms
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Animals
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Inhibitory Concentration 50
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Integrin alpha4beta1 / antagonists & inhibitors*
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Integrin alpha4beta1 / blood
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Mice
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Models, Chemical
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Molecular Conformation
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Phenylalanine / chemistry*
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Protein Binding
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Pyridines / chemistry*
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Rats
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Structure-Activity Relationship
Substances
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Integrin alpha4beta1
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Pyridines
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Phenylalanine