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Synthesis and evaluation of antiinflammatory activity of substituted chalcone derivatives

PDF Downloads : Oriental Journal of Chemistry

Joshi RS, Mandhane PG, Diwakar SD, Dabhade SK, Gill CH. Synthesis, analgesic and anti-inflammatory activities of some novel pyrazolines derivatives. Bioorg Med Chem Lett 2010;20:3721-5.

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Anto RJ, Sukumaran K, Kuttan G, Rao MN, Subbaraju V, Kuttan R. Anticancer and antioxidant activity of synthetic chalcones and related compounds. Cancer Lett 1995;97:33-7.

Ozdemir Z, Kandilci HB, Gümüşel B, Caliş U, Bilgin AA. Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-furyl)-pyrazoline derivatives. Eur J Med Chem 2007;42:373-9.


The anti-inflammatory activity of the synthesized compounds (7ae, 9, 11, 13a, b) and Ibuprofen as a reference drug were screened on Carrageenan-induced hind paw edema model,) at different time intervals (). All screened compounds showed significant reduction in rat paw edema reflecting their anti-inflammatory activity. Notably, the percent inhibition reached its maximum value at the 4th hour, compounds 7d, e, and 13b showed the maximum potency at the 4th hour.

activity of o-allyl chalcone derivatives.

Motivated by these findings coupled with our ongoing program in the field of chalcones and other heterocyclic compounds conducted with them as anti-inflammatory agents.,) In the present work, we decided to synthesize some new chalcones containing benzofuran moiety; in addition, a novel series of fused pyrimidines will be synthesized with a potential to act as dual anti-inflammatory–antibacterial agents with minimal gastrointestinal (GI) side effects and high safety margin.

Journal of Enzyme Inhibition and Medicinal Chemistry: ..

Combination of pharmacophores on the same scaffold is a well established approach to the synthesis of more potent drugs.) Heterocycles containing benzofuran nucleus are known to have a wide range of potent pharmacological activities. Brazilian propolis naturally occurring benzofuran derivatives were found to have mild cytotoxic activity against highly liver-metastatic murine colon 26-L5 carcinoma and human HT-1080 fibrosarcoma cells.) Ailanthoidol has been reported to have antiviral, antioxidant and antifungal activities.) Furthermore, most of compounds prepared from 2-acetylbenzofurans have antimicrobial, antitumor, anti-inflammatory activity, and they are used in treatment of cardiac arrhythmias.–)

Synthesis, antiinflammatory and antibacterial activity ..

The development of an effective therapeutic agent for the management of inflammation has undergone continual evolution leading to the emergence of more efficacious classes of drugs. Chalcones have been synthesized in order to develop drugs active against cancer,,) malaria,,) tuberculosis,) and cardiovascular diseases) or for their properties to modulate the regulation of biochemical pathways like nitric oxide (NO)) or tyrosine kinase.)

chalcone/flavone derivatives 3a-e

Background and aim: Spiroazetidin-2-ones and furans are commonly used as anti-bacterial, anti-fungal, anti-inflammatory, cardiovascular activities, anticancer, antiparkinson agents etc. The purpose of this study was to perform virtual toxicity studies of the synthesized compounds 1-(substitutedphenyl)-3-chloro-5,9-bis(furan-2-ylmethylidene)-1-azaspiro[3.5]nonan-2-ones (3a-3h). Materials and method...