Literature DB >> 29407945

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

Chantal Barberot1, Aurélie Moniot2, Ingrid Allart-Simon1, Laurette Malleret3, Tatiana Yegorova4, Marie Laronze-Cochard1, Abderrazzaq Bentaher3, Maurice Médebielle5, Jean-Philippe Bouillon4, Eric Hénon1, Janos Sapi1, Frédéric Velard2, Stéphane Gérard6.   

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.
Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Entities:  

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

Mesh：

Substances：

Year:  2018        PMID： 29407945     DOI： 10.1016/j.ejmech.2018.01.035

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  6 in total

1.  Pyridazinones and Structurally Related Derivatives with Anti-Inflammatory Activity.

Authors:  Niccolo Cantini; Igor A Schepetkin; Nadezhda V Danilenko; Andrei I Khlebnikov; Letizia Crocetti; Maria Paola Giovannoni; Liliya N Kirpotina; Mark T Quinn
Journal:  Molecules       Date:  2022-06-10       Impact factor: 4.927

2.  Inhibition of Recruitment and Activation of Neutrophils by Pyridazinone-Scaffold-Based Compounds.

Authors:  Aurélie Moniot; Julien Braux; Renaud Siboni; Christine Guillaume; Sandra Audonnet; Ingrid Allart-Simon; Janos Sapi; Rabindra Tirouvanziam; Stéphane Gérard; Sophie C Gangloff; Frédéric Velard
Journal:  Int J Mol Sci       Date:  2022-06-29       Impact factor: 6.208

3.  Discovery of 3,6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico insights.

Authors:  Ahmed Sabt; Wagdy M Eldehna; Tarfah Al-Warhi; Ohoud J Alotaibi; Mahmoud M Elaasser; Howayda Suliman; Hatem A Abdel-Aziz
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

4.  Synthesis and biological evaluation of a new series of ortho-carboranyl biphenyloxime derivatives.

Authors:  Guofan Jin; Fuyan Xiao; Ruijiang Liu
Journal:  Chem Cent J       Date:  2018-06-29       Impact factor: 4.215

5.  Pyridazinone Derivatives Limit Osteosarcoma-Cells Growth In Vitro and In Vivo.

Authors:  Aurélie Moniot; Julien Braux; Camille Bour; Christine Guillaume; Fabien Lamret; Ingrid Allart-Simon; Sandra Audonnet; Sarah Renault; Francoise Rédini; Marie Laronze-Cochard; Janos Sapi; Sophie C Gangloff; Stéphane Gérard; Frédéric Velard
Journal:  Cancers (Basel)       Date:  2021-11-28       Impact factor: 6.639

6.  Pyridazinone derivatives as potential anti-inflammatory agents: synthesis and biological evaluation as PDE4 inhibitors.

Authors:  Ingrid Allart-Simon; Aurélie Moniot; Nicolo Bisi; Miguel Ponce-Vargas; Sandra Audonnet; Marie Laronze-Cochard; Janos Sapi; Eric Hénon; Frédéric Velard; Stéphane Gérard
Journal:  RSC Med Chem       Date:  2021-03-01
  6 in total

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