Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists.
Bioorg Med Chem Lett
; 20(24): 7327-30, 2010 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-21074434
ABSTRACT
Bicyclic piperazine derivatives were synthesized as conformationally constrained analogs of N-alkyl piperazines and were found to be potent CB1 receptor agonists. The CB1 receptor agonist activity was dependent upon the absolute configuration of the chiral center of the bicyclic ring system. Although the conformational constraint did not protect the compounds from metabolism by N-dealkylation, several bicyclic analogs were found to be more potent than the unconstrained lead compound. Compound 8b demonstrated potent antinociceptive activity in vivo.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Compostos Bicíclicos com Pontes
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Receptor CB1 de Canabinoide
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Compostos Azabicíclicos
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Amidas
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Indóis
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article