Difluoroketones as inhibitors of matrix metalloprotease-13.
Substrate-like difluoroketones have been prepared as potential inhibitors of MMP-13. Weak inhibition was seen with the key target 2. This and the more potent activity of intermediate 7b illustrates that hydrated ketones can be used to inhibit MMP-13 and perhaps other members of this class of enzymes.
Pfizer Inc., Central Research Division, Groton, CT 06340, USA. lawrence_a_reiter@groton.pfizer.com
L A
LA
Reiter
G J
GJ
Martinelli
L A
LA
Reeves
P G
PG
Mitchell
D015195:Drug Design; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D053509:Matrix Metalloproteinase 13; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D007659:Ketones; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D053509:Matrix Metalloproteinase 13