PMID: 6987141Jan 1, 1980Paper

Synthetic inhibitors of serine proteinases. 22. Inhibition of acrosin by benzamidine derivatives

Hoppe-Seyler's Zeitschrift für physiologische Chemie
J Stürzebecher, F Markwardt

Abstract

A series of substituted benzamidines was tested for their inhibitory effects on boar acrosin. Substituents with electron-donating properties and small aliphatic residues increase the inhibitory activity of benzamidine, whereas aromatic residues have only a slight enhancing influence. Only substituents with a beta- or gamma-keto group increase the acrosin binding affinity by more than one order of magnitude. Comparison of the structure-activity relationships for the inhibition of acrosin and trypsin showed differences in the binding sites of both enzymes.

References

Nov 1, 1978·Journal of Medicinal Chemistry·R F ParrishF M Stevens
Dec 1, 1975·Hoppe-Seyler's Zeitschrift für physiologische Chemie·W D SchleuningH Fritz
May 1, 1976·Journal of Reproduction and Fertility·A K BhattacharyyaJ Travis
Jan 1, 1974·Annual Review of Biochemistry·R A McRorie, W L Williams

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Citations

Jun 1, 1984·The Journal of Surgical Research·R IzquierdoR A Prinz
Apr 29, 1980·Biochemical and Biophysical Research Communications·F H Bernhardt, H U Meisch

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