A new group of 4-(Imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitro anti breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 value...

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 ...

a new group of 4-(imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl cox-2 pharmacophore at the para position of the c-2 phenyl ring were designed and synthesized as selective cox-2 inhibitors and in-vitro anti breast cancer agents. in-vitro cox-1 and cox-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the cox-2 isozyme with ic50 value...

As a continuous research for discovery of new COX-2 inhibitors, chemical synthesis, in vitro biological activity and molecular docking study of anew group of 1,4-dihydropyridine (DHP) derivatives were presented. Novel synthesized compounds possessing a COX-2 SO2Me pharmacophore at the para position of C-4 phenyl ring, different hydrophobic groups (R1) at C-2 position and alkoxycarbonyl groups (...

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...

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...