Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.
Bioorg Med Chem Lett
; 12(20): 2887-91, 2002 Oct 21.
Article
em En
| MEDLINE
| ID: mdl-12270170
ABSTRACT
Cathepsin K is highly expressed in human osteoclasts, and is implicated in bone resorption. This makes it an attractive target for the treatment of osteoporosis. Peptides containing 2-amino-1'-hydroxymethyl ketones and 2-amino-1'-alkoxymethyl ketones were discovered as potent inhibitors of cathepsin K. A novel synthetic route was devised to facilitate rapid elucidation of the SAR of these inhibitors. The synthesis and SAR of hydroxymethyl ketones are presented.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Inibidores de Proteases
/
Catepsinas
/
Cetonas
Limite:
Humans
Idioma:
En
Ano de publicação:
2002
Tipo de documento:
Article