Synthesis and Anti-inflammatory Activity of Some Benzofuran and Benzopyran-4-one Derivatives
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Date
2011
Journal Title
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Article
Publisher
Chemical and Pharmaceutical Bulletin
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Abstract
New series of furosalicylic acids 3a—c, furosalicylanilides 6a—n, furobenzoxazines 8a—f, 1-benzofuran-
3-arylprop-2-en-1-ones 12a,b, 6-(aryl-3-oxoprop-1-enyl)-4H-chromen-4-ones 16a—c and 6-[6-aryl-2-thioxo-
2,5-dihydropyrimidin-4-yl]-4H-chromen-4-ones 17a—c were synthesized. Anti-inflammatory activity
evaluation was performed using carrageenan-induced paw edema model in rats and prostaglandin E2 (PGE2)
synthesis inhibition activity. Some of the tested compounds revealed comparable activity with less ulcerogenic
effect than Diclofenac at a dose 100 mg/kg. All the synthesized compounds were docked on the active
site of cyclooxygenase-2 (COX-2) enzyme and most of them showed good interactions with the amino acids of
the active site comparable to the interactions exhibited by Diclofenac.
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Keywords
anti-inflammatory activity, prostaglandin E2, benzofuran, enzopyran-4-one
Citation
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