Design, synthesis and biological evaluation of potent FAAH inhibitors.
Bioorg Med Chem Lett
; 26(11): 2701-5, 2016 06 01.
Article
em En
| MEDLINE
| ID: mdl-27117424
ABSTRACT
A new series of 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and evaluated for their biological activity. Different pharmacomodulations have been explored and the lipophilicity of these compounds was assessed. Investigation of the in vitro biological activity led to the identification of 5 compounds as potent FAAH inhibitors, their good FAAH inhibition capacity is probably correlated with their suitable lipophilicity. Specifically, compound 25 showed similar inhibition potency against FAAH in comparison with URB597, one of the most potent FAAH inhibitor known to date.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Inibidores Enzimáticos
/
Amidoidrolases
/
Isoxazóis
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article