Identification of a bioactive impurity in a commercial sample of 6-methyl-2-p-tolylaminobenzo[d][1,3]oxazin-4-one (URB754).
Ann Chim
; 97(9): 887-94, 2007 Sep.
Article
em En
| MEDLINE
| ID: mdl-17970304
ABSTRACT
The compound URB754 was recently identified as a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) by screening of a commercial chemical library. Based on HPLC/MS, NMR and EI/MS analyses, the present paper shows that the MGL-inhibitory activity attributed to URB754 is in fact due to a chemical impurity present in the commercial sample, identified as bis(methylthio)mercurane. Although this organomercurial compound is highly potent at inhibiting MGL (IC50 = 11.9 +/- 1.1 nM), its biological use is prohibited by its toxicity and target promiscuity.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzoxazinas
/
Compostos de Anilina
Tipo de estudo:
Diagnostic_studies
Idioma:
En
Revista:
Ann Chim
Ano de publicação:
2007
Tipo de documento:
Article