Paper
Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents.
Published Oct 1, 1990 · P. Ting, J. Kaminski, M. Sherlock
Journal of medicinal chemistry
30
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Abstract
A series of analogues based on the 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one ring system have been synthesized and shown to possess oral antiinflammatory activity in both the reverse passive Arthus reaction (RPAR) pleural cavity assay in rats and in the adjuvant-induced arthritic rat model (AAR). Several members of this series additionally exhibit an inhibitory effect on the in vivo production of prostaglandin- and leukotriene-derived products or arachidonic acid metabolism although these compounds exhibit no significant inhibitory activity against the cyclooxygenase and 5-lipoxygenase enzymes in vitro. Structure-activity relationships in this series are discussed.
Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones show oral antiinflammatory activity in a rat model and inhibit prostaglandin and leukotriene production, but show no significant inhibitory activity against cyclooxygena
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