Aldose reductase is a key enzyme in the development of long term diabetic complications and its inhibition represents a viable therapeutic solution for people affected by these pathologies. Therefore, the search for effective aldose reductase inhibitors is a timely and pressing challenge. Herein we describe the access to a novel class of oxyimino derivatives, obtained by reaction of a 1,5-dicarbonyl substrate with O-(arylmethyl)hydroxylamines. The synthesised compounds proved to be active against the target enzyme. The best performing inhibitor, compound (Z)-8, proved also to reduce both cell death and the apoptotic process when tested in an in vitro model of diabetic retinopathy made of photoreceptor-like 661w cell line exposed to high-glucose medium, counteracting oxidative stress triggered by hyperglycaemic conditions.

中文翻译：

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氧亚氨基糖精衍生物是醛糖还原酶抑制剂的一种新型结构类别，具有抗氧化活性。

醛糖还原酶是长期糖尿病并发症发展中的关键酶，其抑制作用为受这些病理影响的人提供了可行的治疗方案。因此，寻找有效的醛糖还原酶抑制剂是一个及时而紧迫的挑战。在本文中，我们描述了通过1,5-二羰基底物与O-（芳基甲基）羟胺反应获得的一类新型的氧亚氨基衍生物。已证明合成的化合物对目标酶具有活性。当在由暴露于高糖培养基的感光受体样661w细胞系制成的糖尿病性视网膜病变的体外模型中测试时，性能最好的抑制剂化合物（Z）-8还可降低细胞死亡和凋亡过程。高血糖症引发的压力。