Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases.
Bioorg Med Chem
; 15(6): 2368-74, 2007 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-17267227
ABSTRACT
Among other non-antibiotic properties, tetracyclines inhibit matrix metalloproteinases and are currently under study for the treatment of osteoarthritis. Quaternary ammonium conjugates of tetracyclines were synthesized by direct alkylation of the amine function at the 4-position with methyl iodide. When tested in vitro, they inhibited cytokine-induced MMP expression to a lesser extent than parent tetracyclines. This was compensated by an improved inhibition of MMP catalytic activity. Since inhibition of collagen degradation was maintained these derivatives could be potent drug candidates for cartilage-targeted chondroprotective treatment.
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Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Tetraciclinas
/
Inibidores de Metaloproteinases de Matriz
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article