A novel series of highly selective inhibitors of MMP-3.
Bioorg Med Chem Lett
; 17(24): 6750-3, 2007 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-18029177
ABSTRACT
The design and synthesis of a series of highly selective hydroxamate inhibitors of stromelysin-1 (MMP-3) is described. Substitution of a 4-biaryl piperidine sulfonamide core, which binds at the S1' subsite of MMP-3, was optimised to give potent inhibitors of MMP-3, with greater than 300-fold selectivity over MMP-1, MMP-2, MMP-9 and MMP-14. Compounds 26 and 27 were identified as having the best balance of pharmacology and properties required for topical drug delivery.
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Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Sulfonamidas
/
Inibidores de Metaloproteinases de Matriz
/
Ácidos Hidroxâmicos
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article