Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.
Bioorg Med Chem Lett
; 20(3): 1237-40, 2010 Feb 01.
Article
in En
| MEDLINE
| ID: mdl-20042333
ABSTRACT
Using a focused screen of biogenic amine compounds we identified a novel series of H(3)R antagonists. A preliminary SAR study led to reduction of MW while increasing binding affinity and potency. Optimization of the physical properties of the series led to (S)-6n, with improved brain to plasma exposure and efficacy in both water intake and novel object recognition models.
Full text:
1
Database:
MEDLINE
Main subject:
Pyrrolidines
/
Benzamides
/
Benzimidazoles
/
Receptors, Histamine H3
/
Histamine H3 Antagonists
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2010
Type:
Article
Affiliation country:
United States