title: New 4(1H)-pyridinone derivatives as analgesic agents.
abstract: A number of 2-methyl/ethyl-3-hydroxy-4(1H)-pyridinones have been synthesized by reacting with 4-pyrones and primary aromatic amines in ethanol. Their structures were confirmed by microanalysis, IR and 1H-NMR spectral analysis. Possible analgesic and anti-inflammatory activities of the synthesized compounds were investigated by acetic acid-induced writhing and carrageenan rat paw edema tests. All compounds exhibited higher analgesic activities than acetylsalicylic acid, 1-(2-Piperidinoethyl)-2- methyl-3-hydroxy-4-(1H)-pyridinone.2HBr(1), 1-[2-(1-methyl-pyrrolidine-2- yl)-ethyl]-2- methyl-3-hydroxy-4(1H)-pyridinone.2HBr (3) and 1-[2-(1-methyl-pyrrolidine- 2-yl)-ethyl]-2- ethyl-3-hydroxy-4(1H)-pyridinone.2HBr (6) showed higher anti-inflammatory activities than indometacin.
authors.affiliation: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
authors.forename: M D
authors.initials: MD
authors.lastname: Aytemir
authors.forename: T
authors.initials: T
authors.lastname: Uzbay
authors.forename: D D
authors.initials: DD
authors.lastname: Erol
mesh_terms: D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
chemical_list: D018712:Analgesics, Non-Narcotic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011728:Pyridones; D002351:Carrageenan