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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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

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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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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-[8-(3-nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acid	3',5'-cyclic-AMP phosphodiesterase 4A	IC 50 (nM)	88	N/A	N/A	Details
4-[8-(3-nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acid	3',5'-cyclic-AMP phosphodiesterase 4B	IC 50 (nM)	49	N/A	N/A	Details
4-[8-(3-nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acid	3',5'-cyclic-AMP phosphodiesterase 4D	IC 50 (nM)	1	N/A	N/A	Details