title: Synthesis and structure-activity relationship studies of quinoxaline derivatives as aldose reductase inhibitors.
abstract: ARIs for diabetes: A series of 2-(3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid derivatives were designed and synthesized as inhibitors of aldose reductase (AR), a novel target for the treatment of diabetes complications. Most of the derivatives proved to be potent and selective, with IC50 values in the low nanomolar to micromolar range.
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China).
authors.forename: Bobin
authors.initials: B
authors.lastname: Wu
authors.forename: Yanchun
authors.initials: Y
authors.lastname: Yang
authors.forename: Xiangyu
authors.initials: X
authors.lastname: Qin
authors.forename: Shuzhen
authors.initials: S
authors.lastname: Zhang
authors.forename: Chaojun
authors.initials: C
authors.lastname: Jing
authors.forename: Changjin
authors.initials: C
authors.lastname: Zhu
authors.forename: Bing
authors.initials: B
authors.lastname: Ma
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001665:Binding Sites; D020134:Catalytic Domain; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D062105:Molecular Docking Simulation; D011485:Protein Binding; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011810:Quinoxalines; C576693:Akr1b1 protein, rat; D000449:Aldehyde Reductase
keywords: aldehyde reductases; aldose reductases; diabetes complications; inhibitors; polyol pathway; quinoxalines; structure-activity relationships