A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

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 ...

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 ...

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 series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

Objective(s):This study was carried out to investigate the effects of COX-2 selective inhibitor (Celecoxib) or non-selective COX inhibitor (Ibuprofen) on gastrointestinal motility. Materials and Methods: The rats were randomly divided into five groups including: intact, sham, traumatic brain injury (TBI) group (intact rats under TBI), Celecoxib group (10 mg/kg), Ibuprofen group (10 mg/kg). Rats...

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 (...

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 (...

objective(s):this study was carried out to investigate the effects of cox-2 selective inhibitor (celecoxib) or non-selective cox inhibitor (ibuprofen) on gastrointestinal motility. materials and methods: the rats were randomly divided into five groups including: intact, sham, traumatic brain injury (tbi) group (intact rats under tbi), celecoxib group (10 mg/kg), ibuprofen group (10 mg/kg). rats...