New synthetic inhibitors of chymotrypsin.
4-Substituted carbonylphenyl ester derivatives were prepared and their inhibitory effects on chymotrypsin, trypsin, thrombin, plasmin, pancreatic kallikrein, and plasma kallikrein were examined. Among the various inhibitors tested, 4-[2-(dimethylamino)ethylaminocarbonyl]phenyl 1,2,3,4-tetrahydro-1-naphthoate hydrochloride (FK-316), 4-[(2-[4-pyrrolidinocarbonylmethyl)oxycarbonyl]-phenyl 5-methoxyindole-3-acetate dihydrochloride (FK-375), 4-[(2-[4-(piperidinocarbonylmethylpiperadino]ethyl)oxycarbonyl+ ++]phenyl 1-naphthylacetate dihydrochloride (FK-386), 4-[(2-[4-(2-[morpholino]ethyl)piperadino]ethyl)oxycarbonyl]p henyl 5-methoxy-2-methylindole-3-acetate trihydrochloride (FK-401) and 4-(4-isopropylpiperadinocarbonyl)phenyl 1,2,3,4-tetrahydro-1-naphthoate methanesulfonate (FK-448) were the most effective and specific inhibitors of chymotrypsin.
D000818:Animals; D002417:Cattle; D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D003956:Dialysis; D005029:Ethylenediamines / Q000494:pharmacology; D007700:Kinetics; D010879:Piperazines / Q000494:pharmacology; D011480:Protease Inhibitors / Q000494:pharmacology*; D013379:Substrate Specificity; D014106:Tosylarginine Methyl Ester / Q000378:metabolism; D014443:Tyrosine / Q000031:analogs & derivatives / Q000378:metabolism
D005029:Ethylenediamines; D010879:Piperazines; D011480:Protease Inhibitors; D014443:Tyrosine; C041234:FK 316; C007651:ethyl N-alpha-acetyl-tyrosinate; C041232:FK 401; C041231:FK 375; C041233:FK 386; C041230:FK 448; D014106:Tosylarginine Methyl Ester; D002918:Chymotrypsin