Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors.
Bioorg Med Chem Lett
; 15(11): 2857-60, 2005 Jun 02.
Article
en En
| MEDLINE
| ID: mdl-15911268
ABSTRACT
Excessive calpain activations contribute to serious cellular damage and have been found in many pathological conditions. Novel chromone carboxamides derived from ketoamides were prepared and evaluated for mu-calpain inhibition. Among synthesized, compound 2i was the most potent calpain inhibitor with an IC(50) value of 0.24 +/- 0.11 microM comparable to the activity of peptide aldehyde calpain inhibitor MDL 28,170. Furthermore, compound 2i showed higher selectivity for mu-calpain over two related cysteine proteases cathepsin B and cathepsin L, suggesting the chromone ring as a good scaffold for selective mu-calpain inhibitors.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Calpaína
/
Inhibidores de Cisteína Proteinasa
/
Cromonas
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2005
Tipo del documento:
Article