Amide Derivatives of [6-(5-Methyl-3-phenylpyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic Acids as Potential Analgesic and Anti-Inflammatory Compounds
| Autor: | M. Fethi Şahin, Erdem Yesilada, Serdar Uenlue, Cagla Akoglu, Erden Banoglu, Esra Kuepeli |
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| Rok vydání: | 2004 |
| Předmět: |
Male
medicine.drug_class Stereochemistry Indomethacin Analgesic Administration Oral Pain Quantitative Structure-Activity Relationship Pharmaceutical Science Acetates Carrageenan Medicinal chemistry Chemical synthesis Anti-inflammatory Mice Acetic acid chemistry.chemical_compound In vivo Amide Drug Discovery Benzoquinones medicine Animals Edema Humans Pain Measurement Analgesics Aspirin Molecular Structure biology Anti-Inflammatory Agents Non-Steroidal Membrane Proteins General Medicine Amides Hindlimb Isoenzymes Pyridazines chemistry Cyclooxygenase 2 Prostaglandin-Endoperoxide Synthases Enzyme inhibitor Cyclooxygenase 1 biology.protein Cyclooxygenase Injections Intraperitoneal |
| Zdroj: | Archiv der Pharmazie. 337:7-14 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.200200738 |
| Popis: | In this study, amide derivatives of [6-(5-methyl-3-phenyl-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were synthesized and tested for their in vivo analgesic and anti-inflammatory activity by using the p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds 6a, 6d, 6e, 6g, 6 h and 6 m were more potent than that of aspirin as an analgesic and indomethacin as an anti-inflammatory drug, respectively. The other derivatives generally resulted in comparable activity to reference compounds. Inhibitor activity of the active compounds on cyclooxygenase isoforms was also investigated by using in vitro human whole blood assay and found that these derivatives did not exert their analgesic and anti-inflammatory activities. through COX inhibition and other mechanisms might be involved. |
| Databáze: | OpenAIRE |
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