Selective, orally active MMP inhibitors with an aryl backbone.
This letter describes SAR exploration and rat PK optimization of a series of novel, MMP-1 sparing aryl hydroxamate sulfonamides with activity against MMP-2 and MMP-13.
Barta
T E
TE
Pharmacia, Department of Medicinal Chemistry, 4901 Searle Parkway, Skokie, IL 60077, USA. barta@netmug.org
Becker
D P
DP
Bedell
L J
LJ
De Crescenzo
G A
GA
McDonald
J J
JJ
Mehta
P
P
Munie
G E
GE
Villamil
C I
CI
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D015195:Drug Design; D053509:Matrix Metalloproteinase 13; D061965:Matrix Metalloproteinase Inhibitors; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry* / Q000494:pharmacology*
D061965:Matrix Metalloproteinase Inhibitors; D010880:Piperidines; D011480:Protease Inhibitors; D013438:Sulfhydryl Compounds; D053509:Matrix Metalloproteinase 13; C507083:Mmp13 protein, rat