2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.
Bioorg Med Chem Lett
; 17(9): 2643-8, 2007 May 01.
Article
em En
| MEDLINE
| ID: mdl-17314044
ABSTRACT
This report describes the effect of replacing the central basic amine present in many known 5-HT(2A) ligands with an aromatic residue. We targeted the isomeric phenethylpyridines 2 and 3 and these compounds proved to be excellent leads, possessing good 5-HT(2A) receptor binding affinity and selectivity over the 5-HT(2C) subtype. Optimization of one isomer led to the identification of 25, a compound with sub-nanomolar 5-HT(2A) affinity and selectivity over 5-HT(2C) of greater than 4600-fold.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Antagonistas da Serotonina
/
Química Farmacêutica
/
Receptor 5-HT2A de Serotonina
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2007
Tipo de documento:
Article