Peptidyl carbamate esters: a new class of specific elastase inhibitors.
A series of tripeptide carbamate esters were synthesized and tested for inhibitory activity towards porcine pancreatic elastase, trypsin and chymotrypsin. Two of these compounds specifically inhibited elastase [Ki = 4.25 x 10(-5)M and 3.00 x 10(-5)M], and exhibited no effect toward the other two serine proteases. These active tripeptidyl carbamates represent a novel class of specific elastase inhibitors.
D000818:Animals; D002219:Carbamates / Q000138:chemical synthesis* / Q000494:pharmacology; D002918:Chymotrypsin / Q000037:antagonists & inhibitors; D007202:Indicators and Reagents; D007700:Kinetics; D010179:Pancreas / Q000201:enzymology; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D011480:Protease Inhibitors / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D013552:Swine; D014361:Trypsin Inhibitors / Q000138:chemical synthesis
D002219:Carbamates; D007202:Indicators and Reagents; D010455:Peptides; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; D002918:Chymotrypsin; D010196:Pancreatic Elastase