Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors

Saghir Hussain, Shagufta Parveen, Xin Hao, Shuzhen Zhang, Wei Wang, Xiangyu Qin, Yanchun Yang, Xin Chen, Shaojuan Zhu, Changjin Zhu*, Bing Ma

*此作品的通讯作者

科研成果: 期刊稿件文章同行评审

126 引用 (Scopus)

摘要

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.

源语言英语
页(从-至)383-392
页数10
期刊European Journal of Medicinal Chemistry
80
DOI
出版状态已出版 - 10 6月 2014

指纹

探究 'Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors' 的科研主题。它们共同构成独一无二的指纹。

引用此