We report here the preclinical profile of etoricoxib (MK-0663) [5-chloro-2-(6-methylpyridin-3-yl)-3-(4-methylsulfonylphenyl)
pyridine], a novel orally active agent that selectively inhibits …

… S. Boyce and N. Rupniak … All right.s reserved. … C.; Brideau, C.; Charleson, S.;
Cromlish, W.; Ethier, D.; Evans, JF; Ford-Hutchinson, AW; Gauthier, JY; Gordon, R.; Guay, J.; …

BACKGROUND & AIMS: In the gastrointestinal tract, prostaglandins are implicated as important
mediators of normal physiological processes. Prostaglandin G/H synthase (PGHS) is the …

The discoveries that cyclooxygenase (COX)-2 is an inducible form of COX involved in
inflammation and that COX-1 is the major isoform responsible for the production of prostaglandins (…

The intracellular distribution of the enzyme 5-lipoxygenase (5-LO) and 5-lipoxygenase-activating
protein (FLAP) in resting and ionophore-activated human leukocytes has been …

… k 2 value of 0.11±0.06 s −1 for the first order rate constant for formation of a tightly bound
enzyme‐inhibitor complex. Comparable values of 62±26 μM and 0.06±0.01 s −1 , respectively, …

… 5-Lipoxygenase-activating protein (FLAP) is an 1 S-kDa integral membrane protein which is
… However, the mechanism by which FLAP activates S-LO has not been determined. We have …

A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and
evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and …

… The inhibition by flurbiprofen was stereoselective, the (S)-flurbiprofen being 600-fold more
… IC50 values ranged from 0.6 nM for (S)-flurbiprofen to 500 µM for salicylic acid. L-745,296, a …

A series of potent and highly selective cyclooxygenase-2 inhibitors have been prepared by
replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending …