Abstract | BACKGROUND: RESULTS: A novel series of N-substituted 2,4-diaminopteridines has been synthesized and evaluated as antioxidants in several assays. Many exhibited potent lipid antioxidant properties, and some are inhibitors of soybean lipoxygenase, IC50 values extending down to 100 nM for both targets. Several pteridine derivatives showed efficacy at 0.01 mmol/kg with little tissue damage in a rat model of colitis. 2-(4-methylpiperazin-1-yl)-N-(thiophen-2-ylmethyl)pteridin-4-amine (18f) at 0.01 mmol/kg exhibited potent anti-inflammatory activity (reduction by 41%). CONCLUSION:
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Authors | Eleni Pontiki, Dimitra Hadjipavlou-Litina, Alexandros Patsilinakos, Trang M Tran, Charles M Marson |
Journal | Future medicinal chemistry
(Future Med Chem)
Vol. 7
Issue 14
Pg. 1937-51
( 2015)
ISSN: 1756-8927 [Electronic] England |
PMID | 26423719
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- 2,4-diaminopteridine
- Anti-Inflammatory Agents
- Diamines
- Free Radical Scavengers
- Lipoxygenase Inhibitors
- Pteridines
- Reactive Oxygen Species
- Lipoxygenase
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Topics |
- Animals
- Anti-Inflammatory Agents
(chemistry, metabolism, therapeutic use)
- Binding Sites
- Colitis
(drug therapy, pathology)
- Diamines
(chemistry)
- Disease Models, Animal
- Edema
(pathology, prevention & control)
- Free Radical Scavengers
(chemistry, metabolism)
- Lipoxygenase
(chemistry, metabolism)
- Lipoxygenase Inhibitors
(chemistry, metabolism, therapeutic use)
- Male
- Molecular Docking Simulation
- Protein Binding
- Protein Structure, Tertiary
- Pteridines
(chemistry, metabolism, therapeutic use)
- Rats
- Reactive Oxygen Species
(chemistry, metabolism)
- Soybeans
(enzymology)
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