Substituted isatoic anhydrides: selective inactivators of trypsin-like serine proteases.
Substituted isatoic anhydrides: selective inactivators of trypsin-like serine proteases.
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DOI：
10.1021/jm00154a026
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发表时间：
1986-04
影响因子：
7.3
通讯作者：
Michael H. Gelb;R. Abeles
中科院分区：
文献类型：
--
作者：
Michael H. Gelb;R. Abeles
靛红酸酐的衍生物的制备和测试作为丝氨酸蛋白酶的抑制剂。一些靛红酸酐与带正电荷的取代基不可逆地灭活几种胰蛋白酶样酶，并优先灭活胰蛋白酶胰凝乳蛋白酶。通过在靛红酸酐的N-1位上引入芳族基团，获得了进一步的选择性。制备了7-（氨甲基）-1-苄基靛红酸酐，并且其是凝血酶的选择性灭活剂;因此可以制备靛红酸酐的衍生物，其具有高度的酶选择性而不连接肽识别结构。
Derivatives of isatoic anhydride were prepared and tested as inhibitors of serine proteases. A number of isatoic anhydrides with positively charged substituents irreversibly inactivated several trypsin-like enzymes and preferentially inactivated trypsin over chymotrypsin. Further selectivity was obtained by introduction of an aromatic group on the N-1 position of isatoic anhydride. 7-(Aminomethyl)-1-benzylisatoic anhydride was prepared and was a selective inactivator of thrombin; thus it is possible to prepare derivatives of isatoic anhydride that are highly enzyme selective without attaching peptide recognition structures.