Abstract
SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series of VLA-4 integrin antagonists are described.
MeSH terms
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Amines / chemistry
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Animals
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Anti-Allergic Agents / antagonists & inhibitors*
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Cyclobutanes / chemical synthesis*
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Cyclobutanes / pharmacology*
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Integrin alpha4beta1
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Integrin beta1
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Integrins / antagonists & inhibitors*
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Metabolic Clearance Rate
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Rats
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Receptors, Lymphocyte Homing / antagonists & inhibitors*
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Receptors, Very Late Antigen
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Structure-Activity Relationship
Substances
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Amines
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Anti-Allergic Agents
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Cyclobutanes
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Integrin alpha4beta1
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Integrin beta1
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Integrins
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Receptors, Lymphocyte Homing
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Receptors, Very Late Antigen
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squaric acid