title: Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents.
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.
authors: Department of Chemistry, Schering-Plough Research, Bloomfield, New Jersey 07003.
authors: P C
authors: PC
authors: Ting
authors: J J
authors: JJ
authors: Kaminski
authors: M H
authors: MH
authors: Sherlock
authors: W C
authors: WC
authors: Tom
authors: J F
authors: JF
authors: Lee
authors: R W
authors: RW
authors: Bryant
authors: A S
authors: AS
authors: Watnick
authors: A T
authors: AT
authors: McPhail
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D001169:Arthritis, Experimental / Q000188:drug therapy; D001183:Arthus Reaction; D001792:Blood Platelets / Q000201:enzymology; D016861:Cyclooxygenase Inhibitors; D004341:Drug Evaluation; D006801:Humans; D066298:In Vitro Techniques; D016859:Lipoxygenase Inhibitors; D009504:Neutrophils / Q000201:enzymology; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors; D011728:Pyridones; D011758:Pyrroles