Tsuji K, Agha B J, Shinogi M, Digenis G A
Biochem Biophys Res Commun. 1984 Jul 31;122(2):571-6. doi: 10.1016/s0006-291x(84)80071-6.
A series of tripeptide carbamate esters were synthesized and tested for inhibitory activity towards porcine pancreatic elastase, trypsin and chymotrypsin. Two of these compounds specifically inhibited elastase [Ki = 4.25 x 10(-5)M and 3.00 x 10(-5)M], and exhibited no effect toward the other two serine proteases. These active tripeptidyl carbamates represent a novel class of specific elastase inhibitors.
合成了一系列三肽氨基甲酸酯,并测试了它们对猪胰弹性蛋白酶、胰蛋白酶和胰凝乳蛋白酶的抑制活性。其中两种化合物特异性抑制弹性蛋白酶(Ki = 4.25×10⁻⁵M和3.00×10⁻⁵M),对其他两种丝氨酸蛋白酶无作用。这些活性三肽基氨基甲酸酯代表了一类新型的特异性弹性蛋白酶抑制剂。