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.

Article Details

Citation

Hersperger R, Dawson J, Mueller T

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.

PubMed ID
11755362 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
4-[8-(3-nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acidcAMP-specific 3',5'-cyclic phosphodiesterase 4AIC 50 (nM)88N/AN/ADetails
4-[8-(3-nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acidcAMP-specific 3',5'-cyclic phosphodiesterase 4BIC 50 (nM)49N/AN/ADetails
4-[8-(3-nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acidcAMP-specific 3',5'-cyclic phosphodiesterase 4DIC 50 (nM)1N/AN/ADetails