New indole amide derivatives as potent CRTH2 receptor antagonists.
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.
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