Phosphodiesterase inhibitors. Part 6: Design, synthesis, and structure–activity relationships of PDE4-inhibitory pyrazolo[1,5-a]pyridines with anti-inflammatory activity
| Autor: | Yuichi Yageta, Yasushi Kohno, Koji Ochiai, Satoshi Takita, Tatsunobu Sumiya, Akira Ohinata, Tokutaro Yasue, Akihiko Kojima, Kazuhiko Iwase, Tetsuya Kishi |
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| Rok vydání: | 2013 |
| Předmět: |
Pyridines
Stereochemistry medicine.drug_class Clinical Biochemistry Phosphodiesterase 3 Anti-Inflammatory Agents Pharmaceutical Science Inhibitory postsynaptic potential Biochemistry Anti-inflammatory Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Animal model Drug Discovery medicine Animals PDE4 Inhibitors Molecular Biology Trifluoromethyl Molecular Structure Chemistry Organic Chemistry Phosphodiesterase Rats Enzyme Activation Design synthesis Drug Design Models Animal Pyrazoles Molecular Medicine Phosphodiesterase 4 Inhibitors |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 23:5311-5316 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2013.07.069 |
| Popis: | We previously identified KCA-1490 [(−)-6-(7-methoxy-2-trifluoromethyl-pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone], a dual PDE3/4 inhibitor. In the present study, we found highly potent selective PDE4 inhibitors derived from the structure of KCA-1490. Among them, N-(3,5-dichloropyridin-4-yl)-7-methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridine-4-carboxamide (2a) had good anti-inflammatory effects in an animal model. |
| Databáze: | OpenAIRE |
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