2. Academic Validation
  3. 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

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

Affiliation

  • 1 Novartis Pharma AG, Arthritis & Bone Metabolism, CH-4002 Basel, Switzerland. rene.hersperger@pharma.novartis.com
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.

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