Design, synthesis and activity evaluation of novel matrix metalloproteinases inhibitors based on the structure of enzyme / 药学学报
Acta Pharmaceutica Sinica
; (12): 1271-1281, 2007.
Article
in Zh
| WPRIM
| ID: wpr-268192
Responsible library:
WPRO
ABSTRACT
A novel inhibitor series for matrix metalloproteinases (MMPs) were designed and synthesized. Using succinate and malonate as zinc binding groups and long hydrophobic substituents to bind with S1' pockets, the compounds showed micromolar inhibition and selectivity for MMP-2 over others. And we found a better activity compound. It is a chance to find a better precursor of MMP-2 inhibitors with activity and bioavailability by further optimization of compounds.
Full text:
1
Index:
WPRIM
Main subject:
Structure-Activity Relationship
/
Drug Design
/
Molecular Structure
/
Chemistry
/
Matrix Metalloproteinases
/
Enzyme Inhibitors
/
Matrix Metalloproteinase Inhibitors
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2007
Type:
Article