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

European Journal of Medicinal Chemistry, ISSN: 0223-5234, Vol: 80, Page: 383-392
2014
  • 127
    Citations
  • 0
    Usage
  • 20
    Captures
  • 0
    Mentions
  • 1
    Social Media
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Metrics Details

  • Citations
    127
  • Captures
    20
  • Social Media
    1
    • Shares, Likes & Comments
      1
      • Facebook
        1

Article Description

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 IC 50 values from low micromolar to submicromolar, and compound 15a bearing a C3-phenethyl side chain was identified as the most potent inhibitor with an IC 50 value of 0.143 μM. The structure–activity studies suggested that both C3-phenethyl and C6-NO 2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors.

Bibliographic Details

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

Elsevier BV

Pharmacology, Toxicology and Pharmaceutics; Chemistry

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