Abstract
Substituted thiazolidinones were identified as CCR4 antagonists from high throughput screening. Subsequent lead optimization efforts resulted in defined structure-activity relationships and the identification of potent antagonists (compounds 90 and 91) that inhibited the chemotaxis of Th2 T-cells in vitro.
MeSH terms
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Animals
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Mice
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Protein Binding / physiology
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Receptors, CCR4
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Receptors, Chemokine / antagonists & inhibitors*
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Receptors, Chemokine / metabolism
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Structure-Activity Relationship
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Thiazolidinediones / chemistry*
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Thiazolidinediones / metabolism
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Thiazolidinediones / pharmacology
Substances
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Ccr4 protein, mouse
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Receptors, CCR4
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Receptors, Chemokine
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Thiazolidinediones