1.
Bioorg Med Chem Lett
; 21(1): 528-30, 2011 Jan 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21111619
RESUMO
A new MMP12 inhibitor series has been identified containing a thiophene moiety. Different approaches have been considered to replace this potential toxicophore. α-Fluorothiophene derivatives were the most interesting compounds. Their synthesis is presented.
Assuntos
Inibidores de Metaloproteinases de Matriz , Inibidores de Proteases/química , Tiofenos/química , Metaloproteinase 12 da Matriz/metabolismo , Inibidores de Proteases/síntese química , Inibidores de Proteases/farmacologia , Relação Estrutura-Atividade , Tiofenos/síntese química , Tiofenos/farmacologia
2.
Bioorg Med Chem Lett
; 15(16): 3787-90, 2005 Aug 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16002291
RESUMO
A new class of MMP-12 inhibitors was discovered and optimized using structure-based drug design methods. Modeling studies using a known MMP-12 crystal structure identified a new interaction mode for these new MMP-12 inhibitors. Further optimization resulted in the discovery of a compound displaying nanomolar activity against MMP-12 and which was co-crystallized with MMP-12.