An aromatic amide of indomethacin recently reported to be a potent and selective reversible inhibitor of COX-2. Inhibits human recombinant COX-2 with IC50 of 0.1 uM.
n-(3-pyridyl)-indomethacin amide is a reversible, potent and selective cox-2 inhibitor [1].cyclooxygenase (cox) is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. cox-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (gi) and of the proaggregatory thromboxane in blood platelets. cox-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. cox-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1].n-(3-pyridyl)-indomethacin amide (n-3pyia) is a reversible, potent and selective cox-2 inhibitor that inhibits human recombinant cox-2 and ovine cox-1 with ic50 values of 0.052 and >66 μm, respectively. it is over 1300 times less potent as an inhibitor of ovine cox-1. n-(3-pyridyl)-indomethacin amide is the 3-pyridyl amide derivative of indomethacin that shows selective against cox-2 [1].
[1]. kalgutkar as, marnett ab, crews bc, et al. ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. j med chem. 2000 jul 27;43(15):2860-70.
