| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371007 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave as a full antagonists, exhibiting good selectivity over related prostaglandin receptors. Also, prototypical compounds in this novel series which displayed acceptable CYP profiles and were orally bioavailable in rats were identified.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Helmi Zaghdane, Michael Boyd, John Colucci, Daniel Simard, Carl Berthelette, Yves Leblanc, Zhaoyin Wang, Robert Houle, Jean François Lévesque, Carmela Molinaro, Martine Hamel, Rino Stocco, Nicole Sawyer, Susan Sillaots, François Gervais, Michel Gallant,