Hamilton R, Walker B, Walker B J
School of Chemistry, Queen's University of Belfast, Northern Ireland.
Bioorg Med Chem Lett. 1998 Jul 7;8(13):1655-60. doi: 10.1016/s0960-894x(98)00272-8.
The synthesis of diphenyl phosphonate analogues of aspartic and glutamic acid, and their inhibitory activity against S. aureus V8 protease and granzyme B, is described. The study has revealed difficulties with protecting group compatibility in the synthesis of these analogues. Two analogues, Acetyl. AspP (OPh)2 and Acetyl.GluP (OPh)2 were found to function as irreversible inactivators of V8 proteinase, yet exhibit no activity against granzyme B.
本文描述了天冬氨酸和谷氨酸的二苯基膦酸酯类似物的合成，以及它们对金黄色葡萄球菌V8蛋白酶和颗粒酶B的抑制活性。该研究揭示了在这些类似物的合成中保护基相容性方面存在的困难。发现两种类似物，即乙酰基-天冬氨酸二苯基膦酸酯（Acetyl. AspP (OPh)2）和乙酰基-谷氨酸二苯基膦酸酯（Acetyl.GluP (OPh)2）可作为V8蛋白酶的不可逆失活剂，但对颗粒酶B无活性。
