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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.

Citation

S Fujii, T Yokoyama, K Ikegaya, N Yokoo. New synthetic inhibitors of chymotrypsin. Journal of biochemistry. 1984 Feb;95(2):319-22

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PMID: 6715301

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