In this work, isatin was employed as the scaffold to design aldose reductase inhibitors with antioxidant activity. Most of the isatin derivatives were proved to be excellent in the inhibition of aldose reductase (ALR2) with IC₅₀ values at submicromolar level, and (E)-2-(5-(4-methoxystyryl)-2,3-dioxoindolin-1-yl) acetic acid (9g) was identified as the most effective with an IC₅₀ value of 0.015 μM. Moreover, compounds 9a–h with styryl side chains at the C5 position of isatin showed potent antioxidant activity. Particularly, the phenolic compound 9h demonstrated similar antioxidant activity with the well-known antioxidant Trolox. Structure-activity relationship and molecular docking studies showed that the acetic acid group at N1 and C5 p-hydroxystyryl side chain were the key structures to increase the aldose reductase inhibitory activity and antioxidant activity.

在这项工作中，靛红被用作支架来设计具有抗氧化活性的醛糖还原酶抑制剂。大多数靛红衍生物在抑制醛糖还原酶 (ALR2) 方面表现出色，IC ₅₀值在亚微摩尔水平，( E )-2-(5-(4-甲氧基苯乙烯基)-2,3-二氧吲哚-1 -yl) 乙酸(9g ) 被鉴定为最有效，IC ₅₀值为 0.015 μM。此外，在靛红 C5 位具有苯乙烯基侧链的化合物9a - h显示出有效的抗氧化活性。特别是酚类化合物9h表现出与众所周知的抗氧化剂 Trolox 相似的抗氧化活性。构效关系和分子对接研究表明，N1和C5对羟基苯乙烯基侧链的乙酸基团是提高醛糖还原酶抑制活性和抗氧化活性的关键结构。