Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1, 7-naphthyridines: a novel class of potent and selective phosphodiesterase type …

R Hersperger, K Bray-French, L Mazzoni…

Index: Hersperger, Rene; Bray-French, Katharine; Mazzoni, Lazzaro; Mueller, Thomas Journal of Medicinal Chemistry, 2000 , vol. 43, # 4 p. 675 - 682

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Citation Number: 48

Abstract

Recently, four subtypes of the human phosphodiesterase type 4 (PDE4A-D) enzyme have been described. So far, only very few PDE4 subtype-selective inhibitors are known. Herein, we describe the synthesis of 6, 8-disubstituted 1, 7-naphthyridines and their characterization as potent and selective inhibitors of PDE4D which suppress the oxidative burst in human eosinophils with IC50 values as low as 0.7 nM. SAR development and the extended use ...