Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4ß2α5 nicotinic acetylcholine receptors.
Bioorg Med Chem Lett
; 24(2): 674-8, 2014 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-24365158
ABSTRACT
The design and synthesis of a series of substituted heteroaromatic α4ß2α5 positive allosteric modulators is reported. The optimization and development of the heteroaromatic series was carried out from NS9283, and several potent analogues, such as 3-(5-(pyridin-3-yl)-2H-tetrazol-2-yl)benzonitrile (5k) and 3,3'-(2H-tetrazole-2,5-diyl)dipyridine (12 h) with good in vitro efficacy were discovered.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores Nicotínicos
/
Antagonistas Nicotínicos
/
Agonistas Nicotínicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Estados Unidos