Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.
Eur J Med Chem
; 45(2): 752-9, 2010 Feb.
Article
em En
| MEDLINE
| ID: mdl-19954866
ABSTRACT
An easy and convenient microwave-assisted synthesis of a small library of indolic arylpiperazine derivatives is described. Parallel and mixed pool combinatorial methods are reported and compared. The described reactions are nucleophilic substitutions of several aromatic piperazines in presence of K(2)CO(3). Good yields and short reaction times are the main aspect of these procedures. Binding assays shed additional light on the influence of the LCAPs on the 5-HT(1A), 5-HT(2A) and 5-HT(2C) receptors affinity and allowed to disclose three interesting compounds as 5-HT(2C), mixed 5-HT(2A)/5-HT(2C) and 5-HT(1A)/5-HT(2C) ligands (4i, 4l and 4d, respectively), with potential antiepileptic, anxiolytic or atypical antipsychotic agent therapeutical profiles.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Serotonina
/
Técnicas de Química Combinatória
/
Indóis
/
Micro-Ondas
Limite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Itália
País de publicação:
FR
/
FRANCE
/
FRANCIA
/
FRANÇA