Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.
Bioorg Med Chem Lett
; 23(13): 3927-34, 2013 Jul 01.
Article
em En
| MEDLINE
| ID: mdl-23692872
ABSTRACT
A novel series of α4ß2 nAChR agonists lacking common pyridine or its bioisosteric heterocycle have been disclosed. Essential pharmacophoric elements of the series are exocyclic carbonyl moiety as a hydrogen bond acceptor and secondary amino group within diaza- or azabicyclic scaffold. Computer modeling studies suggested that molecular shape of the ligand also contributes to promotion of agonism. Proof of concept for improving working memory performance in a novel object recognition task has been demonstrated on a representative of the series, 3-propionyl-3,7-diazabicyclo[3.3.0]octane (34).
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Receptores Nicotínicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article