Discovery and evaluation of Cav3.2-selective T-type calcium channel blockers.
Bioorg Med Chem Lett
; 27(23): 5326-5331, 2017 12 01.
Article
en En
| MEDLINE
| ID: mdl-29074257
ABSTRACT
We identified and characterized a series of pyrrole amides as potent, selective Cav3.2-blockers. This series culminated with the identification of pyrrole amides 13b and 26d, with excellent potencies and/or selectivities toward the Cav3.1- and Cav3.3-channels. These compounds display poor physicochemical and DMPK properties, making their use difficult for in vivo applications. Nevertheless, they are well-suited for in vitro studies.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirroles
/
Bloqueadores de los Canales de Calcio
/
Canales de Calcio Tipo T
/
Descubrimiento de Drogas
/
Amidas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2017
Tipo del documento:
Article