1.
Bioorg Med Chem Lett
; 15(23): 5176-81, 2005 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16185867
RESUMO
Dipeptide-derived alpha-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC(50) values down to 25nM and exhibit greatly improved activity in muscle cells compared to the reference compound MDL28170. Several novel calpain inhibitors have shown positive effects on histological parameters in an animal model of Duchenne muscular dystrophy demonstrating their potential as a treatment option for this fatal disease.