ChemInform Abstract: 1‐Substituted 4‐Aryl‐5‐pyridinylimidazoles: A New Class of Cytokine Suppressive Drugs with Low 5‐Lipoxygenase and Cyclooxygenase Inhibitory Potency.

Abstract

hibitory Potency. -A series of title compounds, e.g. (VII), is synthesized and tested for the ability to bind a recently discovered protein kinase termed CSBP ( CSAID binding protein) and to inhibit lipopolysaccharide-stimulated TNF production in mice. As one of the more potent inhibitors of TNF biosynthesis in mice, (VII) is inactive as an inhibitor of the enzymes 5-LO and PGHS-1 and decreases disease severity in the AA rat model of arthritis. The results suggest that the CSAID class of drugs may afford antiarthritic agents which treat the underlying disease process.-(BOEHM, J. C.; SMIETANA, J. M.; SORENSON, M. E.; GARIGIPATI, R. S.; GALLAGHER, T. F.; SHELDRAKE, P. L.; BRADBEER, J.; BADGER, A. M.; LAYDON, J. T.; LEE, J. C.; HILLEGASS, L. M.; GRISWOLD, D. E.; BRETON, J. J.; CHABOT-FLECHTER, M. C.; ADAMS, J. L.; J.