1.
Bioorg Med Chem Lett
; 19(16): 4546-50, 2009 Aug 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19625186
RESUMO
Potent 3,4-disubstituted benzofuran P1' MMP-13 inhibitors have been prepared. Selectivity over MMP-2 was achieved through a substituent at the C4 position of the benzofuran P1' moiety of the molecule. By replacing a backbone benzene with a pyridine and valine with threonine, compounds (e.g., 44) with greatly reduced plasma protein binding were also obtained.
Assuntos
Benzofuranos/química , Inibidores de Metaloproteinases de Matriz , Inibidores de Proteases/química , Animais , Benzofuranos/síntese química , Benzofuranos/farmacologia , Metaloproteinase 13 da Matriz/metabolismo , Metaloproteinase 2 da Matriz/metabolismo , Inibidores de Proteases/síntese química , Inibidores de Proteases/farmacologia , Ligação Proteica , Coelhos , Albumina Sérica/química , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 15(22): 4961-6, 2005 Nov 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16153831
RESUMO
The structure-based design and synthesis of a series of novel biphenyl sulfonamide carboxylic acids as potent MMP-13 inhibitors with selectivity over MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-14, Aggrecanase 1, and TACE are described.