Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Bioorg Med Chem Lett
; 21(6): 1748-53, 2011 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-21316962
ABSTRACT
Novel 3-(1H-indol-3-yl)-1,2,4-oxadiazoles and -thiadiazoles were synthesized and found to be potent CB1 cannabinoid receptor agonists. The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chains attached to the indole and oxadiazole cores, leading to identification of a CB1 receptor agonist with good oral activity in a range of preclinical models of antinociception and antihyperalgesia.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptor CB1 de Canabinoide
/
Compostos Heterocíclicos
Limite:
Animals
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article