A fluorescent probe for protease sensing and based on the “covalent-assembly” principle is reported. The basic rational for this unusual class of chemodosimeters proposed by the Anslyn and Yang groups entails the synthesis of non-fluorophore caged precursors full-stable and reactive towards the targeted analyte. Unlike the first generation of protease-sensitive “covalent-assembly” type probes recently published by ourselves (Org. Biomol. Chem.2017, 15, 2575-2584), the availability of dicyanomethylidenyl and enzyme-labile phenylacetamide moieties within the core structure of mixed bis-aryl ether 2 enables its rapid conversion into a fluorescent pyronin dye at physiological pH and upon activation with penicillin G acylase (PGA). This is real progress towards the practical implementation of this ingenious activation mechanism to the detection of enzymes in their native environment (in cellulo or in vivo).

报道了一种用于蛋白酶检测并基于“共价组装”原理的荧光探针。Anslyn和Yang研究小组提出的这种化学计量表的非同寻常类别的基本原理是必须合成完全稳定且对目标分析物具有反应性的无荧光笼状前体。不同于第一代的蛋白酶敏感最近由自己发布的“共价组装”型探针（有机化学Biomol公司。化学式2017，15，2575年至2584年），和dicyanomethylidenyl酶不稳定苯基乙酰胺结构部分的所述芯结构内的可用性混合双芳基醚2使它能够在生理pH值下以及被青霉素G酰基转移酶（PGA）激活后迅速转变为荧光吡喃染料。这是朝着实际实施这种巧妙的激活机制以检测其天然环境（纤维素或体内）中的酶的真正进展。