4.7 Article

Synthesis and biological evaluation of pyridazinone derivatives as potential anti-inflammatory agents

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

  1. French National Centre for Scientific Research (CNRS)
  2. French Ministry of Higher Education and Research (MESR)
  3. European Regional Development Fund (FEDER)
  4. Regional Council of Champagne-Ardenne (France)
  5. Reims-Metropole
  6. European Union (Europe invests in Champagne-Ardenne)
  7. Fonds Agir pour les Maladies Chroniques
  8. European Union (European Regional Development Fund)
  9. [ANR-11-EMMA-028-03-03]

向作者/读者索取更多资源

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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