Synthesis of 1,5-diarylpyrazol-3-propanoic acids towards inhibition of cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4 formation
| Autor: | Luis Labeaga, Francisco Ledo, Gretchen Bain, Burcu Çaliskan Ergün, Maria Teresa Nuñe, Bilge Çakir, Janice Darlington, Erden Banoglu |
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| Jazyk: | angličtina |
| Rok vydání: | 2010 |
| Předmět: |
Magnetic Resonance Spectroscopy
Spectrophotometry Infrared Neutrophils Leukotriene B4 Structure-Activity Relationship chemistry.chemical_compound Lipoxygenase Drug Discovery Cyclooxygenase Inhibitors Lipoxygenase Inhibitors chemistry.chemical_classification Arachidonate 5-Lipoxygenase Cyclooxygenase 2 Inhibitors biology Biological activity In vitro Propanoic acid Enzyme chemistry Eicosanoid Biochemistry Cyclooxygenase 2 Arachidonate 5-lipoxygenase biology.protein Pyrazoles Indicators and Reagents Cyclooxygenase Propionates |
| Popis: | A set of 25 derivatives of 3-[1-(6-substituted-pyridazin-3-yl)-5-(4- substitutedphenyl)-1H-pyrazol-3-yl]propanoic acids has been synthesized and evaluated for their in vitro cyclooxygenase-1/2 (COX-1/ 2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes as well as for their 5-lipoxygenase (5-LO)-mediated LTB4 formation inhibitory activity using an assay with activated human polymorphonuclear leukocytes (PMNL). Among the synthesized compounds, especially 4g showed COX-1 (IC50 = 1.5 μM) and COX-2 (IC50 = 1.6 μM) inhibitory activity, whereas compounds 4b and 4 f resulted in the inhibition of 5-LO-mediated LTB4 formation at 14 μM and 12 μM IC50 values, respectively, without any significant inhibition on COX isoforms. © ECV · Editio Cantor Verlag. |
| Databáze: | OpenAIRE |
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