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Arzneimittelforschung 2009; 59(7): 357-363
DOI: 10.1055/s-0031-1296408
Analgesics · Anti-inflammatories · Antiphlogistics · Antirheumatic Drugs
Editio Cantor Verlag Aulendorf (Germany)

Synthesis and Analgesic and Anti-inflammatory Activity of 6-Phenyl/(4-methylphenyl)-3(2H)-pyridazinon-2-propionamide Derivatives

Mehtap Gökçe
1   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey
,
Meral Şirin Colak
1   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey
,
Esra Kiipeli
2   Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, Ankara, Turkey
,
Mustafa Fethi Şahin
1   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey
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Publikationsverlauf

Publikationsdatum:
13. Dezember 2011 (online)

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Abstract

For reducing gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs) a variety of 6-phenyl/(4-methylphenyl)-3(2H)-pyridazi-non-2-propionamide were synthesized. The structures of these new pyridazinone derivatives were confirmed by their IR, 1H-NMR spectra and elementary analysis. All the new compounds were tested in vivo for their analgesic and anti-inflammatory activities. The analgesic activity of the test compounds was determined by phenylbenzoquinone-induced writhing assay and the anti-inflammatory activity was evaluated by the carrageenan-induced rat paw edema model. 6-Phenyl-3(2H)-pyridazinon-2-yl-[4-(4-fluorophe-nyljpiperazinyl] propanamide IV a-3 was the most active one among the synthesized compounds. Also this compound exhibited most potent anti-inflammatory activity. Acetylsalicylic acid and Indometacin were used as reference drugs. Adverse effects of the compounds were examined on gastric mucosa. None of the compounds showed gastric ulcerogenic effect compared with the reference NSAIDs.

Key words

Arylpiperazines - 3(2H)-Pyridazinone amides, analgesic activity, anti-inflammatory activity
 

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