Synthesis and analgesic and anti-inflammatory activity of ethyl (6-substituted-3 (2H)-pyridazinone-2-yl)acetate derivatives.

Abstract	A number of 6-substituted-3(2H)-pyridazinones and the corresponding methyl (6-substituted-3(2H)-pyridazinone-2-yl)acetate derivatives carrying the arylpiperazinyl structure present in potent antinociceptive agents reported in the literature were synthesized. As part of a programme a series of diverse arylpiperazine derivatives of ethyl (6-substituted-3(2H)-pyridazinone-2-yl)acetate were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. Side effects of the compounds were examined on gastric mucosa. None of the compounds showed gastric ulcerogenic effect compared with reference non-steroidal anti-inflammatory drugs (NSAIDs). On the basis of available data, the structure-activity relationship in the series of ethyl (6-substituted-3(2H)-pyridazinone-2-yl)acetate derivatives was also discussed. When compared to parent 6-substituted-3(2H)-pyridazinones, the new ester derivatives, for example ethyl (6-4-[(2-fluoro)phenyl]piperazine-3(2H)-pyridazinone-2-yl)acetate exhibited better analgesic and anti-inflammatory activity and a lower ulcerogenic effect.
Authors	Yasemin Dündar, Mehtap Gökçe, Esra Küpeli, Mustafa Fethi Sahin
Journal	Arzneimittel-Forschung (Arzneimittelforschung) Vol. 57 Issue 12 Pg. 777-81 ( 2007) ISSN: 0004-4172 [Print] Germany
PMID	18380410 (Publication Type: Journal Article)
Chemical References	Acetates Analgesics Anti-Inflammatory Agents, Non-Steroidal Benzoquinones Indicators and Reagents Pyridazines Solvents quinone Carrageenan
Topics	Acetates (chemical synthesis, pharmacology) Analgesics (chemical synthesis, pharmacology) Animals Anti-Inflammatory Agents, Non-Steroidal (chemical synthesis, pharmacology) Benzoquinones Carrageenan Edema (chemically induced, drug therapy, pathology) Indicators and Reagents Magnetic Resonance Spectroscopy Male Mice Pain Measurement (drug effects) Pyridazines (chemical synthesis, pharmacology) Solvents Spectrophotometry, Infrared Stomach Ulcer (chemically induced, pathology)

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