Stürzebecher J, Markwardt F
Hoppe Seylers Z Physiol Chem. 1980 Jan;361(1):25-9. doi: 10.1515/bchm2.1980.361.1.25.
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.
测试了一系列取代苯甲脒对猪顶体蛋白酶的抑制作用。具有供电子性质的取代基和小的脂肪族残基可提高苯甲脒的抑制活性，而芳香族残基仅有轻微的增强作用。只有具有β-或γ-酮基的取代基能使顶体蛋白酶结合亲和力提高一个以上数量级。对顶体蛋白酶和胰蛋白酶抑制作用的构效关系比较表明，这两种酶的结合位点存在差异。
