Hao, Xin Qi, Gang Ma, Hongxing Zhu, Changjin Han, Zhongfei Novel 2-phenoxypyrido[3,2-<i>b</i>]pyrazin-3(4<i>H</i>)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity <p>To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-<i>b</i>]pyrazin-3(4<i>H</i>)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and 2-(7-chloro-2-(3,5-dihydroxyphenoxy)-3-oxopyrido[3,2-<i>b</i>]pyrazin-4(3<i>H</i>)-yl) acetic acid (<b>4k</b>) was the most active with an IC<sub>50</sub> value of 0.023 µM. Moreover, it was encouraging to find that some derivatives showed strong antioxidant activity, and among them, the phenolic 3,5-dihydroxyl compound <b>4l</b> with 7-bromo in the core structure was proved to be the most potent, even comparable to that of the well-known antioxidant Trolox. Thus the results suggested success in the construction of potent and selective AKR1B1 inhibitors with antioxidant activity.</p> Aldose reductase inhibitor;antioxidant activity;2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one 2019-07-26
    https://tandf.figshare.com/articles/journal_contribution/Novel_2-phenoxypyrido_3_2-_i_b_i_pyrazin-3_4_i_H_i_-one_derivatives_as_potent_and_selective_aldose_reductase_inhibitors_with_antioxidant_activity/9115760
10.6084/m9.figshare.9115760.v1