Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 80, Issue -, Pages 383-392Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.04.047
Keywords
Quinoxalinone derivatives; Aldose reductase inhibitors; Structure-activity relationships
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Funding
- National Natural Science Foundation of China [21272025]
- Research Fund for the Doctoral Program of Higher Education of China [20111101110042]
- Science and Technology Commission of Beijing (China) [Z131100004013003]
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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 mu M. 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. (C) 2014 Elsevier Masson SAS. All rights reserved.
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