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Synonyms: A-64077 | ZYFLO®
zileuton is an approved drug (FDA (1996))
Compound class: Synthetic organic
Comment: Zileuton is an orally active 5-LOX inhibitor.
The approved drug is a racemic mixture of R(+) and S(-) enantiomers (PubChem CID 10681296 and CID 10220327 respectively), which are both pharmacologically active. The structure shown here does not specify stereochemistry and represents the mixture.
The hepatotoxicity of zileuton is suggested to be due to the N-hydroxyurea group .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: zileuton
1. Carter GW, Young PR, Albert DH, Bouska J, Dyer R, Bell RL, Summers JB, Brooks DW. (1991)
5-lipoxygenase inhibitory activity of zileuton.
J Pharmacol Exp Ther, 256 (3): 929-37. [PMID:1848634]
2. Malec J, Przybyszewski WM, Grabarczyk M, Sitarska E. (1984)
Hydroxyurea has the capacity to induce damage to human erythrocytes which can be modified by radical scavengers.
Biochem Biophys Res Commun, 120 (2): 566-73. [PMID:6732772]
3. Prasher P, Pooja, Singh P. (2014)
Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.
Bioorg Med Chem, 22 (5): 1642-8. [PMID:24508141]
4. Sinha S, Doble M, Manju SL. (2018)
Design, synthesis and identification of novel substituted 2-amino thiazole analogues as potential anti-inflammatory agents targeting 5-lipoxygenase.
Eur J Med Chem, 158: 34-50. [PMID:30199704]
5. Zouboulis ChC, Saborowski A, Boschnakow A. (2005)
Zileuton, an oral 5-lipoxygenase inhibitor, directly reduces sebum production.
Dermatology (Basel), 210 (1): 36-8. [PMID:15604543]