Abstract
The synthesis and characterization of 3-formylchromone (1) and its derivatives 2-24 and evaluation of their potential antiinflammatory activities is reported here. These compounds were characterized by (1)H NMR, EI MS, IR, and UV spectroscopic techniques and elemental analysis. The synthesized compounds were evaluated by using various in vitro and in vivo assay models for antiinflammatory activity and their effects were compared with known standard drug such as aspirin and indomethacin. Among all tested compounds, 1, 2, 5, 6, 9, 14, 16-19, 21-23, showed promising antiinflammatory activities. The results and SAR has been discussed in this report.
2010 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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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Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
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Carrageenan / pharmacology
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Chromones / chemical synthesis
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Chromones / chemistry*
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Chromones / pharmacology*
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Chromones / therapeutic use
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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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Cyclooxygenase Inhibitors / therapeutic use
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Edema / chemically induced
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Edema / drug therapy
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Female
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Inflammation / drug therapy
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Male
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Prostaglandin-Endoperoxide Synthases / metabolism
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Rats
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Rats, Wistar
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Respiratory Burst / drug effects
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Xanthine / metabolism
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Xanthine Oxidase / metabolism
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Chromones
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Cyclooxygenase Inhibitors
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formylchromone
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Xanthine
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Carrageenan
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Prostaglandin-Endoperoxide Synthases
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Xanthine Oxidase