Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.
Bioorg Med Chem Lett
; 17(3): 819-22, 2007 Feb 01.
Article
en En
| MEDLINE
| ID: mdl-17107796
ABSTRACT
A direct correlation between hERG binding and QTc prolongation was established for a series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists. Compounds within this class with greater selectivity over hERG were developed. Compound 4h proved to have the best profile, with MCH-R1 Ki = 16 nm and hERG IC50 = 25 microM.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Piperazinas
/
Receptores de Somatostatina
/
Bloqueadores de los Canales de Potasio
/
Canales de Potasio Éter-A-Go-Go
/
Naftalenos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Estados Unidos
