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New indole amide derivatives as potent CRTH2 receptor antagonists

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 selectivit...

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Published in:	Bioorganic & medicinal chemistry letters 2011-06, Vol.21 (11), p.3471-3474
Main Authors:	Zaghdane, Helmi, Boyd, Michael, Colucci, John, Simard, Daniel, Berthelette, Carl, Leblanc, Yves, Wang, Zhaoyin, Houle, Robert, Lévesque, Jean François, Molinaro, Carmela, Hamel, Martine, Stocco, Rino, Sawyer, Nicole, Sillaots, Susan, Gervais, François, Gallant, Michel
Format:	Article
Language:	English
Subjects:	Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals antagonists Asthma Biological and medical sciences blood CRTH2 receptor antagonists DP2 receptor antagonist Histamine and antagonists. Allergy Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Inhibitory Concentration 50 Ligands Medical sciences MK-7246 Molecular Structure Pharmacology. Drug treatments Prostaglandin receptors prostaglandins Protein Binding - drug effects Rats receptors Receptors, Dopamine D2 - agonists Respiratory system
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creator	Zaghdane, Helmi Boyd, Michael Colucci, John Simard, Daniel Berthelette, Carl Leblanc, Yves Wang, Zhaoyin Houle, Robert Lévesque, Jean François Molinaro, Carmela Hamel, Martine Stocco, Rino Sawyer, Nicole Sillaots, Susan Gervais, François Gallant, Michel
description	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.
doi_str_mv	10.1016/j.bmcl.2011.03.085
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subjects	Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals antagonists Asthma Biological and medical sciences blood CRTH2 receptor antagonists DP2 receptor antagonist Histamine and antagonists. Allergy Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Inhibitory Concentration 50 Ligands Medical sciences MK-7246 Molecular Structure Pharmacology. Drug treatments Prostaglandin receptors prostaglandins Protein Binding - drug effects Rats receptors Receptors, Dopamine D2 - agonists Respiratory system
title	New indole amide derivatives as potent CRTH2 receptor antagonists
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