Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-04, Vol.14 (7), p.1619-1624
Main Authors: Allen, Shelley, Newhouse, Bradley, Anderson, Aaron S., Fauber, Benjamin, Allen, Andrew, Chantry, David, Eberhardt, Christine, Odingo, Joshua, Burgess, Laurence E.
Format: Article
Language:English
Subjects:
Allergic diseases
Animals
Biological and medical sciences
Histamine and antagonists. Allergy
Immunopathology
Medical sciences
Mice
Pharmacology. Drug treatments
Protein Binding - physiology
Receptors, CCR4
Receptors, Chemokine - antagonists & inhibitors
Receptors, Chemokine - metabolism
Respiratory and ent allergic diseases
Structure-Activity Relationship
Thiazolidinediones - chemistry
Thiazolidinediones - metabolism
Thiazolidinediones - pharmacology
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.01.072