Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.
Bioorg Med Chem Lett
; 22(8): 2943-7, 2012 Apr 15.
Article
in En
| MEDLINE
| ID: mdl-22424974
New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demonstrated robust weight loss in a diet-induced obese rat model with very low systemic exposure. Pharmacokinetic data suggest that efficacy is primarily driven through activation of CCK1R's located within the intestinal wall.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Piperidines
/
Receptor, Cholecystokinin A
/
Drug Discovery
/
Amides
Limits:
Animals
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Humans
/
Male
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2012
Document type:
Article
Affiliation country:
Country of publication: