Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.
Bioorg Med Chem Lett
; 25(3): 581-6, 2015 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-25556092
ABSTRACT
Through a ligand-based pharmacophore model (S)-proline based compounds were identified as potent cannabinoid receptor 2 (CB2) agonists with high selectivity over the cannabinoid receptor 1 (CB1). Structure-activity relationship investigations for this compound class lead to oxo-proline compounds 21 and 22 which combine an impressive CB1 selectivity profile with good pharmacokinetic properties. In a streptozotocin induced diabetic neuropathy model, 22 demonstrated a dose-dependent reversal of mechanical hyperalgesia.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácido Pirrolidonocarboxílico
/
Prolina
/
Receptor CB2 de Canabinoide
/
Isoxazóis
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article