Novel pyrazole-3-carboxamide derivatives as cannabinoid-1 (CB1) antagonists: journey from non-polar to polar amides.
Bioorg Med Chem Lett
; 21(1): 562-8, 2011 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-21075633
ABSTRACT
The synthesis and biological evaluation of novel pyrazole-3-carboxamide derivatives as CB1 antagonists are described. As a part of eastern amide SAR, various chemically diverse motifs were introduced. In general, a range of modifications were well tolerated. Several molecules with high polar surface area were also identified as potent CB1 receptor antagonists. The in vivo proof of principle for weight loss is exemplified with a lead compound from this series.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Tetrazóis
/
Receptor CB1 de Canabinoide
/
Amidas
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Índia