Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity

A naturally occurring nonaprenylsulfate (1) and its synthetic analogue (2) were synthesized from substituted phenolic precursors in three steps with an overall yield of 40–45%. Both compounds exhibited potent anti-inflammatory activity against 5-lipoxygenase, and potent brine shrimp lethality. They also showed moderate anti-oxidant activity in the super oxide radical scavenging model. Nonaprenylsulfate (1) showed moderate inhibition of paw edema in Freund's Complete Adjuvant (FCA) induced model of arthritis, thus confirming its anti-inflammatory activity.

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Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents

Acta Pharmaceutica ◽

10.2478/v10007-008-0028-x ◽

2008 ◽

Vol 58 (4) ◽

pp. 467-477 ◽

Cited By ~ 11

Author(s):

Mohammad Amir ◽

Sadique Javed ◽

Harish Kumar

Keyword(s):

Lipid Peroxidation ◽

Biological Evaluation ◽

Inflammatory Activity ◽

Test Results ◽

Mass Spectral Data ◽

Standard Drug ◽

Mass Spectral ◽

H Nmr ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents Twelve new 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones (7-18) have been synthesized by reacting 1-aryl-3-(1H-indol-3-yl)-2-propen-1-one with urea and thiourea in ethanolic potassium hydroxide. Their structures have been confirmed by IR, 1H NMR and mass spectral data. The compounds were tested for their anti-inflammatory activity. Test results revealed that compounds showed 49.5 to 70.7% anti-inflammatory activity where-as the standard drug ibuprofen showed 86.4% activity at the same oral dose. Four compounds, 4-(1H-indol-3-yl)-6-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-2-one (8), 4-(1H-indol-3-yl)-6-(4-methylphenyl)-1,2,3,4-tetrahydropyrimidin-2-one (10), 4-(1H-indol-3-yl)-6-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-2-thione (14), 4-(1H-indol-3-yl)-6-(4-methylphenyl)-1,2,3,4-tetrahydropyrimidin-2-thione (16), that showed significant anti-inflammatory activity were selected to study their ulcerogenic and lipid peroxidation activities. All tested compounds showed significant reduction in the ulcerogenic potential and lipid peroxidation compared to the standard drug ibuprofen.

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Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2018.01.068 ◽

2018 ◽

Vol 146 ◽

pp. 381-394 ◽

Cited By ~ 12

Author(s):

Grażyna Chłoń-Rzepa ◽

Agnieszka Jankowska ◽

Marietta Ślusarczyk ◽

Artur Świerczek ◽

Krzysztof Pociecha ◽

...

Keyword(s):

Biological Evaluation ◽

Inflammatory Activity ◽

Design Synthesis ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation ◽

Derivatives Of ◽

Activity Design

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Synthesis and Biological Evaluation of Andrographolide Derivatives as Anti-inflammatory Agent

Current Pharmaceutical Design ◽

10.2174/1381612824666180724130014 ◽

2018 ◽

Vol 24 (30) ◽

pp. 3529-3533 ◽

Cited By ~ 6

Author(s):

Zeyu Zhu ◽

Haibing Duan ◽

Mei Jing ◽

Lipeng Xu ◽

Pei Yu

Keyword(s):

Bacterial Infections ◽

Inflammatory Diseases ◽

Cell Activity ◽

Biological Evaluation ◽

Inflammatory Activity ◽

Special Effects ◽

Inflammatory Drugs ◽

Anti Inflammatory ◽

New Compounds ◽

Synthesis And Biological Evaluation

Background: Andrographolide (Andro) is a main active ingredient of the natural plant Andrographis paniculata, which has special effects on bacterial infections and inflammatory diseases. Objective: We previously synthesized Andrographolide derivatives AL-1 and investigated its anti-inflammatory activity. For further research, we decided to modify the structure of AL-1 and expected to have better antiinflammatory activity. Methods: By conjugating with anti-inflammatory and anti-bacterial group, we designed and synthesized the andrographolide derivative AL-2, AL-3 and AL-4. The anti-inflammatory activity of AL-2, AL-3 and AL-4 was also evaluated by detecting cell activity and Nitric Oxide (NO) release. <p> Results: The new compounds AL-2, AL-3 and AL-4 increased cell viability in lipopolysaccharide (LPS)-induced RAW 264.7 cell, which could have a certain anti-inflammatory activity, and inhibited the release of NO in cells to reduce the inflammatory response of cells. Conclusion: The new compounds AL-2, AL-3 and AL-4 may be candidates of anti-inflammatory drugs in the future.

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