Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.
Bioorg Med Chem Lett
; 13(19): 3375-9, 2003 Oct 06.
Article
in En
| MEDLINE
| ID: mdl-12951129
A series of 4-substituted 8-aryl-2-methylquinolines 4 was designed and synthesized as highly potent antagonists for the human CRF(1) receptor. This series of compounds displayed parallel SAR to other bicyclic systems such as pyrazolo[1,5-a]pyrimidines, with several compounds possessing low nanomolar binding affinity. In addition to the high potency, the basicity of this 4-aminoquinoline core may offer CRF(1) antagonists with lower lipophilicity.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Quinolines
/
Receptors, Corticotropin-Releasing Hormone
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2003
Document type:
Article
Affiliation country:
Estados Unidos
Country of publication:
Reino Unido