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New indole amide derivatives as potent CRTH2 receptor antagonists

Authors :
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
Source :
Bioorganic & Medicinal Chemistry Letters. 21:3471-3474
Publication Year :
2011
Publisher :
Elsevier BV, 2011.

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.

Details

ISSN :
0960894X
Volume :
21
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....a09028c83914f05337f367fe720b7f52
Full Text :
https://doi.org/10.1016/j.bmcl.2011.03.085