Abstract
In the present study, a series of chalcone derivatives were designed based on QSAR analysis. The designed compounds were synthesized by Claisen Schmidt condensation and evaluated for anti-inflammatory, antioxidant and antiulcer activities. The results of the best 2D & 3D QSAR models suggested that by introducing electron releasing groups at R2 and introducing heteroatom with increasing bulkiness at R4 in the benzylideneacetophenone nucleus will increase the activity. The structures of the compounds were established by IR, 1H NMR and mass spectral analysis. All the compounds were evaluated for their anti-inflammatory (carrageenan-induced rat paw edema assay), antioxidant (inhibition of lipid peroxidation) and antiulcer activity (indomethacin-induced gastric damage). Of 10 compounds screened, compounds 1e and 1d exhibited promising anti-inflammatory activity with 68-70% inhibition at 100mg/kg , inhibition of lipid peroxidation with IC50 2.47 & 3.1 μg/ml respectively. The Compounds 1e, 1j and 1d exhibited good gastro protective action as indicated by their low ulcer score. Overall, 1e was obtained as lead compound with promising anti-inflammatory, antioxidant and antiulcer activities.
Keywords: rheumatoid arthritis, NSAIDS, postoperative pain, osteoarthritis, orthopedic injuries, oxidative stress, QSAR Analysis, Reactive oxygen species (ROS), hydroxyl radical (OH.), Chalcones, open-chain flavanoids
Letters in Drug Design & Discovery
Title:Design, Synthesis and Evaluation of Chalcone Derivatives as Anti- Inflammatory, Antioxidant and Antiulcer Agents
Volume: 9 Issue: 5
Author(s): Alka N. Choudhary, Arun Kumar, Vijay Juy
Affiliation:
Keywords: rheumatoid arthritis, NSAIDS, postoperative pain, osteoarthritis, orthopedic injuries, oxidative stress, QSAR Analysis, Reactive oxygen species (ROS), hydroxyl radical (OH.), Chalcones, open-chain flavanoids
Abstract: In the present study, a series of chalcone derivatives were designed based on QSAR analysis. The designed compounds were synthesized by Claisen Schmidt condensation and evaluated for anti-inflammatory, antioxidant and antiulcer activities. The results of the best 2D & 3D QSAR models suggested that by introducing electron releasing groups at R2 and introducing heteroatom with increasing bulkiness at R4 in the benzylideneacetophenone nucleus will increase the activity. The structures of the compounds were established by IR, 1H NMR and mass spectral analysis. All the compounds were evaluated for their anti-inflammatory (carrageenan-induced rat paw edema assay), antioxidant (inhibition of lipid peroxidation) and antiulcer activity (indomethacin-induced gastric damage). Of 10 compounds screened, compounds 1e and 1d exhibited promising anti-inflammatory activity with 68-70% inhibition at 100mg/kg , inhibition of lipid peroxidation with IC50 2.47 & 3.1 μg/ml respectively. The Compounds 1e, 1j and 1d exhibited good gastro protective action as indicated by their low ulcer score. Overall, 1e was obtained as lead compound with promising anti-inflammatory, antioxidant and antiulcer activities.
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Cite this article as:
Alka N. Choudhary, Arun Kumar, Vijay Juy , Design, Synthesis and Evaluation of Chalcone Derivatives as Anti- Inflammatory, Antioxidant and Antiulcer Agents, Letters in Drug Design & Discovery 2012; 9 (5) . https://dx.doi.org/10.2174/157018012800389368
DOI https://dx.doi.org/10.2174/157018012800389368 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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