non-steroidal anti-inflammatory drugs (nsaids) are the competitive inhibitors of cyclooxygenase (cox), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (pgs). their use is associated with the side effects such as gastrointestinal and renal toxicity. the therapeutic anti-inflammatory action of nsaids is produced by the inhibition of cox-2, while the ...

In this study, a new series of 5-substituted 1-benzyl-2-(methylsulfonyl)-1-H-imidazolewith atypical structure-activity relationship was designed, synthesized, and biologicalevaluated as selective cyclooxygenase-2 inhibitors. Docking studies revealed that althoughthe pharmacophoric substitute of the compound 5b, methylsulfonyl group, has been directlyattached to the central ring, it is in the sa...

In this study, a new series of 5-substituted 1-benzyl-2-(methylsulfonyl)-1-H-imidazolewith atypical structure-activity relationship was designed, synthesized, and biologicalevaluated as selective cyclooxygenase-2 inhibitors. Docking studies revealed that althoughthe pharmacophoric substitute of the compound 5b, methylsulfonyl group, has been directlyattached to the central ring, it is in the sa...

Inhibition of cyclooxygenase-2 (COX-2) has been extensively studied as an approach to reduce proinflammatory markers in acute brain diseases, but the anti-neuroinflammatory role cyclooxygenase-1 (COX-1) inhibition rather neglected. We report that m-terphenylamine derivatives are selective COX-1 inhibitors, able block microglia inflammatory response and elicit a neuroprotective effect. These com...

Cyclooxygenase type 1 is constitutively expressed and accounts for synthesis of prostaglandins in the normal gastrointestinal tract. Cyclooxygenase-2 is expressed at sites of inflammation. Selective inhibitors of cyclooxygenase-2 have been suggested to spare gastrointestinal prostaglandin synthesis, and therefore lack the ulcerogenic effects associated with standard nonsteroidal antiinflammator...

design of selective cyclooxygenase-2 (cox-2) inhibitors is still a challenging task because of active site similarities between cox isoenzymes. to help with this issue, we tried to generate a 3d-qsar (3 dimensional quantitative structure activity relationship) model that might reflect the essential features of cox-2 active sites. compounds in a series of resveratrol derivatives inhibitors with ...

Several studies have demonstrated unequivocally that certain nonsteroidal anti-inflammatory drugs (NSAIDs) such as sodium salicylate, sulindac, ibuprofen, and flurbiprofen cause anti-inflammatory and antiproliferative effects independent of cyclooxygenase activity and prostaglandin synthesis inhibition. These effects are mediated through inhibition of certain transcription factors such as NF-ka...