Docking Studies, Synthesis and Biological Evaluation of β-aryl-β-hydroxy Propanoic Acids for Anti-inflammatory Activity

2017 ◽  
Vol 13 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Jelena Savic ◽  
Sanda Dilber ◽  
Marina Milenkovic ◽  
Jelena Kotur-Stevuljevic ◽  
Bojan Markovic ◽  
...  
Keyword(s):  
Docking Studies ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis, Molecular Modelling and Biological Evaluation of Novel Pyrimidine Derivatives as Anti-inflammatory Agents

2020 ◽  
pp. 49-67
Author(s):  
Naglaa Mohamed Ahmed ◽  
Shahira Nofal ◽  
Samir Mohamed Awad
Keyword(s):  
Docking Studies ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Pyrimidine Derivatives ◽  
Reference Drug ◽  
Rat Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1 ◽  
Good Agreement

Aim: As part of ongoing studies in developing new anti-inflammatory agents, 2-thioxo-1,2,3,4-tetrahydropyrimidine derivative 1 was synthesized by direct Biginelli condensation and used for the synthesis of novel series of  pyrimidin-2-thione derivatives  (2a-d to 7a-b). Materials and Methods: All compounds were examined for their anti-inflammatory activity using the carrageenan-induced rat paw edema assay in comparison to ibuprofen, as a reference drug. Molecular docking studies were carried out using SYBLYL-X v.2.1 software. Study Design: A series of pyrimidine derivatives were synthesized by a simple and available method leads to a molecule of promising anti-inflammatory activity, the docking studies show good agreement with anti-inflammatory results. Future researches are recommended to assure the importance of these new derivatives for various applications. Place and Duration of Study: Pharmaceutical Organic Chemistry Department and Pharmacology and Toxicology Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt, between February 2018 and March 2019. Results: Compounds showed 61 to 86% anti-inflammatory activity where-as ibuprofen showed 69% activity. Compounds 2a, 2b, 2c, 2d, 3a, 3b, 3c, 3d, 7a, 7b induced strong anti-inflammatory activity, comparable with that of ibuprofen, they showed significantly difference at 4h post-carrageenan. Compound 3c (86%) showed the best result of edema inhibition in rats. Moreover, compounds 1, 2c and 3c were subjected to in vitro enzyme assay investigations against COX-1 and COX-2. All tested compounds showed higher potency towards COX-2 over COX-1. Compound 3c realized higher potency towards COX-2 (IC50= 0.046 μM) than compounds 1(IC50= 0.21 μM) and 2c (IC50=0.11 μM) as well as ibuprofen (IC50= 43.628 μM). Structure-activity relationship (SAR) has been discussed. Conclusion: A series of pyrimidine derivatives were synthesized by a simple and available method gave a molecule of promising anti-inflammatory activity, the docking studies showed good agreement with anti-inflammatory results.

Synthesis and Biological Evaluation of the Anti-Inflammatory Activity for some Novel Oxpholipin-11D Analogues

2015 ◽  
Vol 11 (7) ◽  
pp. 705-711
Author(s):  
El-Sayed M. Lashine ◽  
Abdel Fattah Haikal ◽  
Mansour E. Abou Kul ◽  
Lina A. Nasrallah ◽  
Ahmed M. Naglah
Keyword(s):  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

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

2019 ◽  
Vol 352 (3) ◽  
pp. 1800298 ◽  
Author(s):  
Marcela Vettorazzi ◽  
Laura Vila ◽  
Santiago Lima ◽  
Lina Acosta ◽  
Felipe Yépes ◽  
...  
Keyword(s):  
Sphingosine Kinase ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Sphingosine Kinase 2 ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Nonaprenylsulfates

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801
Author(s):  
Suryachandra R. Ravada ◽  
Lakshmareddy Emani ◽  
Ganeswara R. Mallula ◽  
Trimurtulu Golakoti
Keyword(s):  
Brine Shrimp ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Synthetic Analogue ◽  
Paw Edema ◽  
Naturally Occurring ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

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.

scholarly journals 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

2008 ◽  
Vol 58 (4) ◽  
pp. 467-477 ◽  
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.

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

2018 ◽  
Vol 24 (30) ◽  
pp. 3529-3533 ◽  
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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