Structure-activity relationship of the ficin hydrolysis of phenyl hippurates. Comparison with papain, actinidin, and bromelain

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Abstract
A study of the hydrolysis of 30 substituted-phenyl hippurates by the enzyme ficin was made. The following quantitative structure-activity relationship (QSAR) has been derived: log 1/Km = 0.79 .pi.''3 + 0.58 .sigma. + 0.28 MR4,5 + 3.70. In this expression, .pi.''3 refers to the more hydrophobic of the 2 m-substituents, and MR4,5 is the molar refractivity of substituents in the 4- and 5-positions of the phenyl ring. This QSAR is compared with those from papain, actinidin, bromelain B and bromelain D. [The continuous advance in enzyme catalysis, kinetics and mechanism are a source of new ideas for medicinal chemists attempting a more rational and efficient way of designing drugs.].