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

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

121 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)383-392
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume80
DOIs
Publication statusPublished - 10 Jun 2014

Keywords

  • Aldose reductase inhibitors
  • Quinoxalinone derivatives
  • Structure-activity relationships

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