期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 146, 期 -, 页码 139-146出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.01.035
关键词
Pyridazinone; Phosphodiesterase inhibitors; Anti-inflammatory; PDE4
资金
- French National Centre for Scientific Research (CNRS)
- French Ministry of Higher Education and Research (MESR)
- European Regional Development Fund (FEDER)
- Regional Council of Champagne-Ardenne (France)
- Reims-Metropole
- European Union (Europe invests in Champagne-Ardenne)
- Fonds Agir pour les Maladies Chroniques
- European Union (European Regional Development Fund)
- [ANR-11-EMMA-028-03-03]
Cyclic nucleotide phosphodiesterase type 4 (PDE4), that controls intracellular level of cyclic nucleotide CAMP, has aroused scientific attention as a suitable target for anti-inflammatory therapy in respiratory diseases. Here we describe the development of two families of pyridazinone derivatives as potential PDE4 inhibitors and their evaluation as anti-inflammatory agents. Among these derivatives, 4,5-dihydropyridazinone representatives possess promising activity, selectivity towards PDE4 isoenzymes and are able to reduce IL-8 production by human primary polymorphonuclear cells. (C) 2018 Elsevier Masson SAS. All rights reserved.
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