The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.

Article Details

Citation

Laughlin SK, Clark MP, Djung JF, Golebiowski A, Brugel TA, Sabat M, Bookland RG, Laufersweiler MJ, VanRens JC, Townes JA, De B, Hsieh LC, Xu SC, Walter RL, Mekel MJ, Janusz MJ

The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.

Bioorg Med Chem Lett. 2005 May 2;15(9):2399-403.

PubMed ID
15837333 [ View in PubMed
]
Abstract

4-Aryl-3-pyridyl and 4-aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-alpha) inhibitors, which contain a novel isoxazolone five-membered heterocyclic core are described. Many showed sub-micromolar activity against lipopolysaccharide-induced TNF-alpha production.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
2-(ETHOXYMETHYL)-4-(4-FLUOROPHENYL)-3-[2-(2-HYDROXYPHENOXY)PYRIMIDIN-4-YL]ISOXAZOL-5(2H)-ONEMitogen-activated protein kinase 14IC 50 (nM)460N/AN/ADetails