4.7 Article

Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity

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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 65, 期 -, 页码 51-59

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.04.056

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Chalcone; Flavanone; Flavone; Anti-inflammatory; Indomethacin; TNF-alpha

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A novel series of synthetic 2'-hydroxychalcones (1a-h), 2'-methoxychalcones (2a-1), flavanones (3a-k) and flavones (4a-f) have been synthesized and evaluated for their anti-inflammatory activity in carrageenan induced rat paw oedema model. Compounds 1a, 1e-g, 2e-g, 3j, and 4f showed potent anti-inflammatory activity comparable to the reference drug indomethacin with insignificant ulceration. Compound 1f showed mild inhibition against the enzymatic activity of ovine COX-1 and COX-2 (in-vitro). Compound 1f also exhibited inhibitory activity in LPS induced TNF-alpha production. (C) 2013 Elsevier Masson SAS. All rights reserved.

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