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 ...

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

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 ...

arthritis refers to different medical conditions associated with disorder of the primary structures that determine joint functions such as bones, cartilage and synovial membranes. drug discovery and delivery to retard the degeneration of joint tissues are challenging. current treatments of different arthritis involves administration of ideal non-steroidal anti-inflammatory drugs (nsaids) but ar...

A group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-2 or C-4 phenyl ring, in conjunction with a C-4 or C-2 phenyl (4-H) or substituted-phenyl ring (4-F,4-Cl,4-Br,4-OMe,4-Me, 4-NO2), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target 5-oxo-1,4,5,6,7,8 hexahydroquino...

a group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a cox-2 so2me pharmacophore at the para position of the c-2 or c-4 phenyl ring, in conjunction with a c-4 or c-2 phenyl (4-h) or substituted-phenyl ring (4-f,4-cl,4-br,4-ome,4-me, 4-no2), were designed for evaluation as selective cyclooxygenase-2 (cox-2) inhibitors. these target 5-oxo-1,4,5,6,7,8 hexahydroquino...

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 point to an important function of cyclooxygenase (cox) and prostaglandin signaling in models of synaptic plasticity which is associated with n-methyl-d-aspartate receptors (nmdars). cyclooxygenase gene is suggested to be an immediate early gene that is tightly regulated in neurons by nmda dependent synaptic activity. nonsteroid antiinflammatory drugs (nsaids) exert their antiinf...

a substantial amount of evidence has proposed an important role for cyclooxygenase-2 (cox-2) enzyme in brain diseases and affiliate disorders. the purpose of this research was studying the effects of cox-2 selective inhibition on haloperidol-induced catatonia in an animal model of drug overdose and parkinson’s disease (pd). in this study, the effect of acute and sub-chronic oral administration ...