New indole amide derivatives as potent CRTH2 receptor antagonists
| Autor: | Robert Houle, Jean François Lévesque, Daniel Simard, François G. Gervais, Carl Berthelette, Carmela Molinaro, Yves Leblanc, Martine Hamel, Michel Gallant, Helmi Zaghdane, Nicole Sawyer, Susan Sillaots, Zhaoyin Wang, Michael J. Boyd, John Colucci, Rino Stocco |
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| Rok vydání: | 2011 |
| Předmět: |
Indoles
Stereochemistry Clinical Biochemistry Pharmaceutical Science Prostaglandin Ligands Biochemistry Chemical synthesis Inhibitory Concentration 50 chemistry.chemical_compound Amide Drug Discovery Animals Receptor Molecular Biology Indole test Molecular Structure biology Receptors Dopamine D2 Chemistry Organic Chemistry Cytochrome P450 Amides Rats biology.protein Molecular Medicine Prostaglandin D2 Selectivity Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:3471-3474 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.03.085 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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