1613082-54-4Relevant articles and documents
Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors
Hussain, Saghir,Parveen, Shagufta,Hao, Xin,Zhang, Shuzhen,Wang, Wei,Qin, Xiangyu,Yang, Yanchun,Chen, Xin,Zhu, Shaojuan,Zhu, Changjin,Ma, Bing
, p. 383 - 392 (2014/05/20)
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.