1.
Bioorg Med Chem Lett
; 19(16): 4546-50, 2009 Aug 15.
Article
in English
| MEDLINE
| ID: mdl-19625186
ABSTRACT
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.
Subject(s)
Benzofurans/chemistry , Matrix Metalloproteinase Inhibitors , Protease Inhibitors/chemistry , Animals , Benzofurans/chemical synthesis , Benzofurans/pharmacology , Matrix Metalloproteinase 13/metabolism , Matrix Metalloproteinase 2/metabolism , Protease Inhibitors/chemical synthesis , Protease Inhibitors/pharmacology , Protein Binding , Rabbits , Serum Albumin/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 15(22): 4961-6, 2005 Nov 15.
Article
in English
| MEDLINE
| ID: mdl-16153831
ABSTRACT
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.
