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New indole amide derivatives as potent CRTH2 receptor antagonists.
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.
Affiliation
  • Zaghdane H; Medicinal Chemistry, Merck Frosst, Center of Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Quebec, Canada H9H 3L1. Zaghdane.helmi@courrier.uqam.ca
Bioorg Med Chem Lett ; 21(11): 3471-4, 2011 Jun 01.
Article in En | MEDLINE | ID: mdl-21515053
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Dopamine D2 / Amides / Indoles Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Dopamine D2 / Amides / Indoles Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article