Abstract
A new series of cyclooxygenase-2(COX-2) inhibitors with naturally occurring flavone as the main skeleton has been synthesized and their biological activities were evaluated for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the desired pharmacokinetic profiles for improved oral anti-inflammatory activity.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Benzopyrans / chemical synthesis*
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Benzopyrans / pharmacology*
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Carrageenan
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Chemical Phenomena
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Chemistry, Physical
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Cyclooxygenase 1
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Cyclooxygenase 2
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors / chemical synthesis*
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Cyclooxygenase Inhibitors / pharmacokinetics
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Cyclooxygenase Inhibitors / pharmacology*
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Edema / chemically induced
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Edema / prevention & control
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Indicators and Reagents
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Isoenzymes / metabolism*
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Male
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Membrane Proteins
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Prostaglandin-Endoperoxide Synthases / metabolism*
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Rats
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Rats, Sprague-Dawley
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Benzopyrans
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors
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Indicators and Reagents
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Isoenzymes
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Membrane Proteins
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Carrageenan
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Cyclooxygenase 1
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Cyclooxygenase 2
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Prostaglandin-Endoperoxide Synthases
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Ptgs1 protein, rat