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Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2014 Jun 10; Vol. 80, pp. 383-92. Date of Electronic Publication: 2014 Apr 21. - Publication Year :
- 2014
-
Abstract
- 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.<br /> (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Aldehyde Reductase chemistry
Aldehyde Reductase metabolism
Catalytic Domain
Enzyme Inhibitors metabolism
Humans
Molecular Docking Simulation
Quinoxalines metabolism
Structure-Activity Relationship
Aldehyde Reductase antagonists & inhibitors
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Quinoxalines chemistry
Quinoxalines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 80
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 24793885
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.04.047