Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.
Bioorg Med Chem Lett
; 14(24): 6011-6, 2004 Dec 20.
Article
en En
| MEDLINE
| ID: mdl-15546719
Several fused bicyclic systems have been investigated to serve as the core structure of potent and selective 5-HT1F receptor agonists. Replacement of the indole nucleus in 2 with indazole and 'inverted' indazole provided more potent and selective 5-HT1F receptor ligands. Indoline and 1,2-benzisoxazole systems also provided potent 5-HT1F receptor agonists, and the 5-HT1A receptor selectivity of the indoline- and 1,2-benzisoxazole-based 5-HT1F receptor agonists could be improved with modification of the benzoyl moiety of the benzamides. Through these studies, we found that the inherent geometries of the templates, not the nature of hybridization of the linking atom, were important for the 5-HT1F receptor recognition.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Benzamidas
/
Receptores de Serotonina
/
Agonistas de Receptores de Serotonina
/
Compuestos Bicíclicos Heterocíclicos con Puentes
Tipo de estudio:
Diagnostic_studies
/
Evaluation_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Reino Unido