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

  • Bioorg Med Chem Lett. 2002 Jan 21;12(2):233-5. doi: 10.1016/s0960-894x(01)00720-x.
Rene Hersperger  1 ,  Janet Dawson ,  Thomas Mueller
Affiliations
  • 1. Novartis Pharma AG, Arthritis & Bone Metabolism, CH-4002 Basel, Switzerland. [email protected]
PMID: 11755362 DOI: 10.1016/s0960-894x(01)00720-x
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.