Synthesis and Analgesic Activity of Some 4,6-Disubstituted-3(2H)-Pyridazinone Derivatives
| Autor: | Murat Suekueroglu, Serdar Uenlue, Erden Banoglu, Esra Kuepeli, Mustafa Fethi Sahin, Erdem Yesilada |
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| Rok vydání: | 2011 |
| Předmět: |
Male
Analgesics Magnetic Resonance Spectroscopy Spectrophotometry Infrared Analgesic Biological activity General Medicine Combinatorial chemistry Medicinal chemistry Pyridazines Mice chemistry.chemical_compound Propanoic acid chemistry In vivo Amide Drug Discovery Benzoquinones Side chain Animals Organic chemistry Indicators and Reagents Stomach Ulcer Pain Measurement |
| Zdroj: | Scopus-Elsevier |
| ISSN: | 1616-7066 0004-4172 |
| Popis: | A series of 6-morpholino-4-aryl-3(2H)-pyridazinone alkanoic acids, their ester and amide derivatives were prepared and tested for their in vivo analgesic activity by using the p-benzoquinone-induced writhing test. The analgesic activity of the compounds 6-morpholino-4-aryl-3(2H)-pyridazinone (6a-b) were comparable but little lower than that of acetyl-salicylic acid (CAS 50-78-2) as an analgesic agent. The 6-morpholino-4-aryl-3(2H)-pyridazinones having a propanoic acid (10a-b), ester (7a) and amides (12a-b, 12d and 12g) as side chains at the position 2 of the pyridazinone ring showed higher activity than the reference compound without gastric ulceration forming potential. All other compounds generally showed higher activity but caused gastric ulceration in the animals. |
| Databáze: | OpenAIRE |
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