Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).
Bioorg Med Chem Lett
; 22(2): 868-71, 2012 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-22217870
ABSTRACT
AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA(2) did not change. Subsequent metal screening experiments determined the inhibition to be Zn(2+) dependent. Structure-activity relationship studies indicated the presence of the 4-hydroxy group to be critical and selected substituted phenyl, polycyclic, and cycloaliphatic amides of xanthurenic acid to be well tolerated.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos Organometálicos
/
Xanturenatos
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Zinco
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1-Alquil-2-acetilglicerofosfocolina Esterase
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Inibidores Enzimáticos
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Amidas
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article