1,5-Disubstituted Indazol-3-ols with Anti-Inflammatory Activity
| Autor: | Ute Egerland, Ilona Dr Fleischhauer, Hildegard Poppe, Szelenyi I, Jürgen Engel, Rudolf Schindler, Norbert Höfgen, Wolfgang Sauer, Sabine Heer, Bernhard Kutscher |
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| Rok vydání: | 1998 |
| Předmět: |
Indazoles
medicine.drug_class Guinea Pigs Pharmaceutical Science In Vitro Techniques Pharmacology Anti-inflammatory Guinea pig Mice chemistry.chemical_compound In vivo Eosinophilia Drug Discovery Tumor Cells Cultured medicine Animals IC50 biology Anti-Inflammatory Agents Non-Steroidal chemistry Enzyme inhibitor Arachidonate 5-lipoxygenase biology.protein Arachidonic acid medicine.symptom |
| Zdroj: | Archiv der Pharmazie. 331:13-21 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/(sici)1521-4184(199801)331:1<13::aid-ardp13>3.0.co;2-m |
| Popis: | A series of new indazol-3-ol derivatives was synthesized. Some of these compounds exhibit interesting anti-inflammatory activities in various models of inflammation. 5-Methoxy-1-[quinoline-2-yl-methoxy)-benzyl]-1H-indazol-3-ol (27) strongly inhibits the oxidation of arachidonic acid to 5-hydroperoxyeicosatetraenoic acid catalyzed by 5-lipoxygenase (IC50 = 44 nM). 27 also inhibits the contraction of sensitized guinea pig tracheal segments (IC50 = 2.9 microM). In guinea pigs treated with 27 (1 mg/kg i.p.) 2 h before antigen provocation, there was a marked inhibition (47%) of the antigen-induced airway eosinophilia. After topical application of 1 microgram/ear 27 inhibits the arachidonic acid induced mouse ear edema (41%). |
| Databáze: | OpenAIRE |
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