New analgesic and antiinflammatory agents 4(1H)-pyridinone derivatives.
A series of 1,2,5-trisubstituted 4(1H)-pyridinone derivatives (7-14) were synthesised by using 4-pyrone derivatives with primary amines in ethanol. The structures of the synthesised compounds were confirmed by analytical and spectral data (UV, IR and 1H-NMR and microanalysis). Analgesic and antiinflammatory activities of the synthesised compounds were investigated by acetic acid-induced writhing syndrome and carrageenan rat paw edema tests. All of the test compounds exhibited higher analgesic activities than acetyl salicylic acid and showed higher antiinflammatory activities than indomethacin. The anti-inflammatory activity and gastric ulceration potential of the compounds were tested using indomethacin as reference drug.
Oztürk
Gülcan
G
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Hacettepe University, 06100 Sihhiye-Ankara, Turkey.
Erol
Dilek Demir
DD
Aytemir
Mutlu Dilsiz
MD
Uzbay
Tayfun
T
D018712:Analgesics, Non-Narcotic / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000704:Analysis of Variance; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D011728:Pyridones / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011728:Pyridones; D002351:Carrageenan