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Eur J Med Chem ; 46(9): 4035-41, 2011 Sep.
Article in English | 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.


Subject(s)
Analgesics, Opioid/chemical synthesis , Analgesics, Opioid/pharmacology , Morphine Derivatives/chemical synthesis , Morphine Derivatives/pharmacology , Analgesics, Opioid/pharmacokinetics , Animals , Blood-Brain Barrier , Magnetic Resonance Spectroscopy , Male , Mice , Morphine Derivatives/pharmacokinetics , Spectrometry, Mass, Electrospray Ionization
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