Synthesis and Structure–Activity Relationship Studies of Quinoxaline Derivatives as Aldose Reductase Inhibitors

Authors

  • Bobin Wu,

    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
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  • Dr. Yanchun Yang,

    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
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  • Dr. Xiangyu Qin,

    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
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  • Dr. Shuzhen Zhang,

    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
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  • Dr. Chaojun Jing,

    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
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  • Prof. Dr. Changjin Zhu,

    Corresponding author
    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
    • Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)

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  • Dr. Bing Ma

    Corresponding author
    1. Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)
    • Department of Applied Chemistry, Beijing Institute of Technology, Zhongguancun South St., 100081 Beijing (China)

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Abstract

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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.

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