Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3.
Structure-activity relationship study and in vitro biochemical studies with human leukocyte elastase, cathepsin G and proteinase 3 were conducted using a series of succinimide derivatives.
Groutas
W C
WC
Department of Chemistry, Wichita State University, KS 67260, USA.
Brubaker
M J
MJ
Chong
L S
LS
Venkataraman
R
R
Huang
H
H
Epp
J B
JB
Kuang
R
R
Hoidal
J R
JR
D000596:Amino Acids / Q000737:chemistry; D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D019272:Leukocyte Elastase; D053146:Myeloblastin; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D012697:Serine Endopeptidases / Q000187:drug effects*; D015842:Serine Proteinase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013388:Succinimides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013997:Time Factors
D000596:Amino Acids; D004791:Enzyme Inhibitors; D015842:Serine Proteinase Inhibitors; D013388:Succinimides; C032620:succinimide; D002403:Cathepsins; D012697:Serine Endopeptidases; C534094:CTSG protein, human; D056649:Cathepsin G; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase; D053146:Myeloblastin