Yokoo, Nobuo published the artcileStudies on synthesis of water-soluble chymotrypsin inhibitors. II, Recommanded Product: 2-(Dimethylamino)-2-oxoethyl 2-(4-hydroxyphenyl)acetate, the publication is Yakugaku Zasshi (1988), 108(5), 443-9, database is CAplus.
Water-soluble, substrate-analogous chymotrypsin inhibitors were synthesized to study the role of chymotrypsin and chymotrypsin-like enzymes in vivo. Ph esters of carboxylic acids containing condensed ring such as tetralin, naphthalene, indole, etc. show potent inhibitory activity against chymotrypsin. Thus, the influence of several substituents on the benzene nucleus of Ph component upon the inhibitory activity against enzymes was investigated. Phenolic esters containing basic substituents in the 4-position exhibited potent inhibition against chymotrypsin, e.g. the IC50 value of 4-amidinophenyl tetralin-1-carboxylate was 5 × 10-7 M. The activity of phenolic esters containing neutral substituents in the 4 position was weaker than that of the basic esters. The IC50 value of the neutral ester, 4-(N,N-dimethylcarbamoylmethoxycarbonylmethyl)phenyl tetralin-1-carboxylate was 7 × 10-6M. Acidic esters with carboxyl groups on the benzene nucleus inhibited most weakly of the three, whose corresponding IC50 value was 6 × 10-5M. A similar tendency was observed in other esters derived from benzoic acid, 1-naphthylacetic acid, 3-indolylacetic acid, etc. The relative order of inhibitory activity of the acyl groups against chymotrypsin was as follows: 5-methoxy-2-methyl-3-indolylacetyl ≥ 1-naphthylacetyl ≥ tetralin-1-carbonyl > 3-indolylacetyl > benzoyl. 4-(4-Guanidinobenzoyloxy)phenyl esters and 4-amidinophenyl esters inhibited not only chymotrypsin but also trypsin. On the other hand, the others, such as 4-(4-isopropylpiperazinocarbonyl)phenyl esters inhibited chymotrypsin specifically.
Yakugaku Zasshi published new progress about 59721-16-3. 59721-16-3 belongs to esters-buliding-blocks, auxiliary class Amine,Benzene,Phenol,Ester,Amide, name is 2-(Dimethylamino)-2-oxoethyl 2-(4-hydroxyphenyl)acetate, and the molecular formula is C8H6F3NO, Recommanded Product: 2-(Dimethylamino)-2-oxoethyl 2-(4-hydroxyphenyl)acetate.
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