Novel inhibitors of procollagen C-terminal proteinase. Part 1: diamino Acid hydroxamates.
The parallel synthesis of novel inhibitors of procollagen C-terminal proteinase is described. The synthetic strategy allowed for the facile synthesis of a large number of side-chain diversified diamino acid hydroxamates, of which the D-diaminopropionic acid derivatives were shown to be single digit nanomolar PCP inhibitors.
Delaet
N G J
NG
CombiChem Inc., 4570 Executive Drive, 92121, San Diego, CA, USA. ndelaet@kemia.com
Robinson
L A
LA
Wilson
D M
DM
Sullivan
R W
RW
Bradley
E K
EK
Dankwardt
S M
SM
Martin
R L
RL
Van Wart
H E
HE
Walker
K A M
KA
D055395:Bone Morphogenetic Protein 1; D019485:Bone Morphogenetic Proteins / Q000037:antagonists & inhibitors*; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007700:Kinetics; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D019485:Bone Morphogenetic Proteins; D006877:Hydroxamic Acids; D007202:Indicators and Reagents; D011480:Protease Inhibitors; D008666:Metalloendopeptidases; D055395:Bone Morphogenetic Protein 1