(2014) Synthesis, biological evaluation and docking study of 3-aroyl-1-(4- sulfamoylphenyl)thiourea derivatives as 15-lipoxygenase inhibitors. European Journal of Medicinal Chemistry. pp. 308-313.
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Abstract
A series of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives containing sulfonamide moiety were designed and synthesized as 15-lipoxygenase (15-LOX) inhibitors. Most synthesized compounds showed potent activity against soybean 15-LOX with IC50 values less than 25 μM. The most potent compound 4c (3-methylbenzoyl derivative) with IC50 value of 1.8 μM was 10-fold more potent than quercetin. Interestingly, compound 4c also showed the highest antioxidant activity, as determined by ferric reducing antioxidant power (FRAP) assay. Its capacity for reducing ferric ion was more than ascorbic acid. The viability assay of the selected compound 4c against oxidative stress-induced cell death in differentiated PC12 cells revealed that compound 4c significantly protected neurons against cell death in low concentrations. © 2014 Elsevier Masson SAS. All rights reserved.
| Item Type: | Article |
|---|---|
| Keywords: | 2 chloro n (4 sulfamoylphenyl)carbamothioylbenzamide; 2 methyl n (4 sulfamoylphenyl)carbamothioylbenzamide; 2,3,4,5 tetrafluoro n (4 sulfamoylphenyl)carbamothioylbenzamide; 2,4 dichloro n (4 sulfamoylphenyl)carbamothioylbenzamide; 3 chloro n (4 sulfamoylphenyl)carbamothioylbenzamide; 3 fluoro n (4 sulfamoylphenyl)carbamothioylbenzamide; 3 methyl n (4 sulfamoylphenyl)carbamothioylbenzamide; 4 chloro n (4 sulfamoylphenyl)carbamothioylbenzamide; 4 methoxy n (4 sulfamoylphenyl)carbamothioylbenzamide; 4 methyl n (4 sulfamoylphenyl)carbamothioylbenzamide; 4 nitro n (4 sulfamoylphenyl)carbamothioylbenzamide; amide; arachidonate 15 lipoxygenase; ascorbic acid; benzamide derivative; enzyme inhibitor; ferric ion; n (4 sulfamoylphenyl)carbamothioyl 2 naphthamide; n (4 sulfamoylphenyl)carbamothioylbenzamide; n (4 sulfamoylphenyl)carbamothioylfuran 2 carboxamide; n (4 sulfamoylphenyl)carbamothioylthiophene 2 carboxamide; quercetin; thiourea derivative; unclassified drug; arachidonate 15 lipoxygenase; hydrogen peroxide; lipoxygenase inhibitor, animal cell; antioxidant activity; article; assay; cell death; cell viability assay; concentration (parameters); drug potency; drug synthesis; enzyme inhibition; ferric reducing antioxidant power assay; IC 50; molecular docking; molecular model; nerve cell; neuroprotection; nonhuman; oxidative stress; PC12 cell line; rat; soybean; animal; antagonists and inhibitors; cell culture; cell differentiation; cell survival; chemical structure; chemistry; dose response; drug effects; enzymology; metabolism; structure activity relation; synthesis, Animals; Arachidonate 15-Lipoxygenase; Cell Death; Cell Differentiation; Cell Survival; Cells, Cultured; Dose-Response Relationship, Drug; Hydrogen Peroxide; Lipoxygenase Inhibitors; Models, Molecular; Molecular Structure; Oxidative Stress; PC12 Cells; Rats; Soybeans; Structure-Activity Relationship |
| Page Range: | pp. 308-313 |
| Journal or Publication Title: | European Journal of Medicinal Chemistry |
| Volume: | 82 |
| Publisher: | Elsevier Masson SAS |
| Depositing User: | ms soheila Bazm |
| URI: | http://eprints.ssu.ac.ir/id/eprint/9071 |
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