4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Bioorg Med Chem Lett
; 18(16): 4642-6, 2008 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-18662880
ABSTRACT
We describe here a novel 4-amino-2-cyanopyrimidine scaffold for nonpeptidomimetic cathepsin S selective inhibitors. Some of the synthesized compounds have sub-nanomolar potency and high selectivity toward cathepsin S along with promising pharmacokinetic and physicochemical properties. The key structural features of the inhibitors consist of a combination of a spiro[2.5]oct-6-ylmethylamine P2 group at the 4-position, a small or polar P3 group at the 5-position and/or a polar group at the 6-position of the pyrimidine.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Pirimidinas
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Catepsinas
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Inibidores de Cisteína Proteinase
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Química Farmacêutica
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Nitrilas
Limite:
Animals
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Humans
/
Male
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article