Abstract
A novel series of synthetic 2'-hydroxychalcones (1a-h), 2'-methoxychalcones (2a-l), 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-α production.
Keywords:
Anti-inflammatory; Chalcone; Flavanone; Flavone; Indomethacin; TNF-α.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Carrageenan
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Cell Line
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Chalcones / chemical synthesis
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Chalcones / chemistry
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Chalcones / pharmacology*
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Cyclooxygenase 1
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Cyclooxygenase 2
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Cyclooxygenase Inhibitors / chemical synthesis
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology*
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Disease Models, Animal
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Dose-Response Relationship, Drug
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Edema / chemically induced
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Edema / drug therapy*
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Female
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Flavanones / chemical synthesis
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Flavanones / chemistry
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Flavanones / pharmacology*
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Flavones / chemical synthesis
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Flavones / chemistry
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Flavones / pharmacology*
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Lipopolysaccharides / antagonists & inhibitors
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Lipopolysaccharides / pharmacology
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Male
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Mice
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Molecular Structure
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Rats
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Rats, Wistar
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Sheep
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Structure-Activity Relationship
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Tumor Necrosis Factor-alpha / biosynthesis
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Chalcones
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Cyclooxygenase Inhibitors
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Flavanones
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Flavones
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Lipopolysaccharides
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Tumor Necrosis Factor-alpha
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Carrageenan
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Cyclooxygenase 1
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Cyclooxygenase 2