Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
Bioorg Med Chem Lett
; 16(3): 746-9, 2006 Feb.
Article
en En
| MEDLINE
| ID: mdl-16321528
ABSTRACT
The SAR of the lead compound 3, a novel ligand for the alpha(2)delta subunit of voltage-gated calcium channels, was rapidly explored. Utilizing a parallel solution-phase Sn2Ar coupling approach, a focused library was obtained. The library was evaluated in vitro and afforded a series of analogues with improved potencies. The SAR trends of the library are also described.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Canales de Calcio
/
Activación del Canal Iónico
/
Técnicas Químicas Combinatorias
/
Subunidades de Proteína
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
Estados Unidos