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Synthesis and biological evaluation of pyridazinone derivatives as potential anti-inflammatory agents. 2018
Chantal Barberot, and
Aurélie Moniot, and
Ingrid Allart-Simon, and
Laurette Malleret, and
Tatiana Yegorova, and
Marie Laronze-Cochard, and
Abderrazzaq Bentaher, and
Maurice Médebielle, and
Jean-Philippe Bouillon, and
Eric Hénon, and
Janos Sapi, and
Frédéric Velard, and
Stéphane Gérard
Université de Reims Champagne-Ardenne, Institut de Chimie Moléculaire de Reims (ICMR), UMR CNRS 7312, UFR Sciences, Moulin de La Housse and UFR Pharmacie, 51 Rue Cognacq-Jay, 51096 Reims, France.
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.
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