Neumann U, Stürzebecher J, Leistner S, Vieweg H
Institute of Pharmacology and Toxicology, Medical Academy Erfurt, G.D.R.
J Enzyme Inhib. 1991;4(3):227-32. doi: 10.3109/14756369109035846.
Eight 3,1-Benzoxazin-4-ones have been used to inactivate chymotrypsin and pancreatic elastase. Whereas 6,7-dimethoxy substitution only slightly decreased the acylation rate constant, the deacylation reaction was nearly unaffected. Bulky alkoxy groups in position 2 of the heterocyclic moiety were shown to increase enormously the acylation rate of chymotrypsin, but not that of elastase.
八种3,1-苯并恶嗪-4-酮已被用于使胰凝乳蛋白酶和胰弹性蛋白酶失活。虽然6,7-二甲氧基取代仅略微降低了酰化速率常数，但脱酰基反应几乎未受影响。杂环部分2位的庞大烷氧基被证明极大地提高了胰凝乳蛋白酶的酰化速率，但对弹性蛋白酶的酰化速率没有影响。
