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Pyridazinone derivatives as potential anti-inflammatory agents: synthesis and biological evaluation as PDE4 inhibitors. 2021
Ingrid Allart-Simon, and
Aurélie Moniot, and
Nicolo Bisi, and
Miguel Ponce-Vargas, and
Sandra Audonnet, and
Marie Laronze-Cochard, and
Janos Sapi, and
Eric Hénon, 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 F-51096 Reims France stephane.gerard@univ-reims.fr.
Cyclic nucleotide phosphodiesterase type 4 (PDE4), which controls the intracellular level of cyclic adenosine monophosphate (cAMP), has aroused scientific attention as a suitable target for anti-inflammatory therapy of respiratory diseases. This work describes the development and characterization of pyridazinone derivatives bearing an indole moiety as potential PDE4 inhibitors and their evaluation as anti-inflammatory agents. Among these derivatives, 4-(5-methoxy-1H-indol-3-yl)-6-methylpyridazin-3(2H)-one possesses promising activity, and selectivity towards PDE4B isoenzymes and is able to regulate potent pro-inflammatory cytokine and chemokine production by human primary macrophages.
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