Introduction Nepafenac (NEPA), [2-(2-amino 3-benzoyl phenyl) acetamide] (Figure 1) is Antiinflammatory (NSAID’s) which is indicated for the treatment of pain and inflammation associated with cataract surgery. NEPA is a prodrug. After penetrating the cornea, NEPA undergoes rapid bioactivation to amfenac, which is a potent NSAID that uniformly inhibits the COX1 and COX2 activity. [1] Amfenac is t...

Kidney failure is the common end of hypertension and renal diseases. Several authors have suggested that vasodilatory prostaglandins participate in the hemodynamic mechanism responsible for the development of kidney failure. However, the mechanism by which prostaglandins are increased in renal disease is not clear. Recently, 2 isoforms of the enzyme responsible for prostaglandin synthesis, cycl...

This work was performed to investigate structural features of ten models (L1-1L10) pyrrolopyrimidine derivatives in addition evaluating their activity against the cyclooxygenase-2 (COX-2) enzyme target. In this regard, celecoxib (CEL) employed as a reference model for investigated models. Frontier molecular orbitals were evaluated including highest occupied and lowest unoccupied (HOMO LUMO) che...

Human orbital fibroblasts are more susceptible to some actions of proinflammatory cytokines than are fibroblasts from other anatomic regions. These cells produce high levels of PGE(2) when activated by cytokines. Here we report that they express high levels of prostaglandin-endoperoxide H synthase (PGHS)-2, the inflammatory cyclooxygenase, when treated with IL-1beta. This induction results from...

It is well known that administration of non-selective cyclooxygenase (COX) non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk developing gastric and duodenal ulcers. Previously, we reported indomethacin, one these COX drugs, results in acute inflammation small intestine subsequent increased release cytokines, such as interleukin-6 tumor necrosis factor-α, histamines can lead to d...

There are spectral and biochemical data suggesting that a tyrosine group(s) is involved in the cyclooxygenase reaction catalyzed by prostaglandin endoperoxide (PGH) synthase. Treatment with tetranitromethane, a reagent which nitrates tyrosine residues, abolishes cyclooxygenase activity, but this inactivation can be largely prevented by competitive cyclooxygenase inhibitors such as ibuprofen and...