Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
Eur J Med Chem. 2014 Jun 10;80:383-92. doi: 10.1016/j.ejmech.2014.04.047. Epub 2014 Apr 21.
Novel quinoxalinone derivatives were synthesized and tested for their inhibitory activity against aldose reductase. Among them, N1-acetate derivatives had significant activity in a range of IC50 values from low micromolar to submicromolar, and compound 15a bearing a C3-phenethyl side chain was identified as the most potent inhibitor with an IC50 value of 0.143 μM. The structure-activity studies suggested that both C3-phenethyl and C6-NO2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors.
新型喹喔啉酮衍生物被合成并测试其对醛糖还原酶的抑制活性。其中，N1-乙酸酯衍生物在低至亚微摩尔的范围内具有显著的活性，并且具有 C3-苯乙基侧链的化合物 15a 被鉴定为最有效的抑制剂，IC50 值为 0.143 μM。构效关系研究表明，C3-苯乙基和 C6-NO2 基团都对增强基于喹喔啉酮的抑制剂的活性和选择性起着重要作用。
