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. 2018 Feb 25:146:139-146.
doi: 10.1016/j.ejmech.2018.01.035. Epub 2018 Jan 17.

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

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

Chantal Barberot et al. Eur J Med Chem. .

Abstract

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.

Keywords: Anti-inflammatory; PDE4; Phosphodiesterase inhibitors; Pyridazinone.

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