Pyridazinone Derivatives As Potential Anti-inflammatory Agents: Synthesis and Biological Evaluation As PDE4 Inhibitors

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2021 May 28

PMID 34046629

Citations 7

Authors

Ingrid Allart-Simon

Aurelie Moniot

Nicolo Bisi

Miguel Ponce-Vargas

Sandra Audonnet

Marie Laronze-Cochard

Janos Sapi

Eric Henon

Frederic Velard

Stephane Gerard

Affiliations

Soon will be listed here.

Abstract

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-1-indol-3-yl)-6-methylpyridazin-3(2)-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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Pyridazinones and Structurally Related Derivatives with Anti-Inflammatory Activity.

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