Synthesis and biological evaluation of analogues of M6G.
Eur J Med Chem
; 46(9): 4035-41, 2011 Sep.
Article
em En
| MEDLINE
| ID: mdl-21689868
ABSTRACT
Synthesis and biological evaluation of new derivatives of Morphine-6-Glucuronide (M6G) are described. M6G is an active metabolite of morphine which displays more analgesia than morphine with a superior side effect profile but with a less efficiently BBB penetration. These phenomena could be explained by the presence of the glucuronide moiety, which confers a higher hydrophilic character compare to morphine. In this context, we have prepared three analogues of M6G possessing a tetrazole, an oxadiazole, and a triazolopyrimidine moiety instead of the carboxylic acid function on position 5 of the sugar. These three analogues showed higher analgesic properties than morphine and M6G even by oral administration.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Analgésicos Opioides
/
Derivados da Morfina
Limite:
Animals
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article