Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor. |
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| Authors: | Rene Hersperger Janet Dawson Thomas Mueller |
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| Affiliation: | Novartis Pharma AG, Arthritis & Bone Metabolism, CH-4002 Basel, Switzerland. rene.hersperger@pharma.novartis.com |
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| Abstract: | 
The synthesis of a 6,8-disubstituted 1,7-naphthyridine 1 and its characterization as a potent and selective phosphodiesterase type 4D inhibitor (IC(50)=1.5nM) are described. The compound inhibited TNFalpha-release from human peripheral blood mononuclear cells and was orally active in a model of adjuvant-induced arthritis in rats. |
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