Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370805 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
A novel series of biaryl phenoxyacetic acids was discovered as potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). A hit compound 4 was discovered from high throughput screening. Modulation of multiple aryl substituents afforded both agonists and antagonists, with small changes often reversing the mode of action. Understanding the complex SAR allowed design of potent antagonists such as potential candidate 34.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tim Luker, Roger Bonnert, Jerzy Schmidt, Carol Sargent, Stuart W. Paine, Stephen Thom, Gary Pairaudeau, Anil Patel, Rukhsana Mohammed, Elizabeth Akam, Iain Dougall, Andrew M. Davis, Phil Abbott, Steve Brough, Ian Millichip, Thomas McInally,