The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Bioorg Med Chem Lett
; 20(3): 887-92, 2010 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-20061146
ABSTRACT
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo studies using deuterated MK-0674 show stereoselective epimerization of the alcohol stereocenter via an oxidation/reduction cycle. From in vitro incubations, two metabolites could be identified the hydroxyleucine and the glucuronide conjugate which were confirmed using authentic synthetic standards.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Bifenilo
/
Inibidores de Cisteína Proteinase
/
Descoberta de Drogas
/
Catepsina K
Tipo de estudo:
Guideline
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2010
Tipo de documento:
Article