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

R Hersperger, J Dawson, T Mueller

Index: Hersperger, Rene; Dawson, Janet; Mueller, Thomas Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 2 p. 233 - 235

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Citation Number: 25

Abstract

The synthesis of a 6, 8-disubstituted 1, 7-naphthyridine 1 and its characterization as a potent and selective phosphodiesterase type 4D inhibitor (IC50= 1.5 nM) are described. The compound inhibited TNFα-release from human peripheral blood mononuclear cells and was orally active in a model of adjuvant-induced arthritis in rats.

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