Biological evaluation of novel benzisoxazole derivatives as PPARdelta agonists.

Article Details

Citation

Sakuma S, Endo T, Kanda T, Nakamura H, Yamasaki S, Yamakawa T

Biological evaluation of novel benzisoxazole derivatives as PPARdelta agonists.

Bioorg Med Chem. 2011 May 15;19(10):3255-64. doi: 10.1016/j.bmc.2011.03.053. Epub 2011 Mar 31.

PubMed ID
21515063 [ View in PubMed
]
Abstract

We discovered novel peroxisome proliferator-activated receptor delta agonists with a characteristic benzisoxazole ring. Compound 5 exhibited potent human PPARdelta transactivation activity. Furthermore, it stimulated the differentiation of oligodendrocyte precursor cells in vitro. This indicates that this potential drug may be effective for the treatment of demyelinating disorders such as multiple sclerosis.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CardarinePeroxisome proliferator-activated receptor alphaEC 50 (nM)990N/AN/ADetails
CardarinePeroxisome proliferator-activated receptor deltaEC 50 (nM)1.7N/AN/ADetails
GW-590735Peroxisome proliferator-activated receptor alphaEC 50 (nM)10N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor deltaEC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)100N/AN/ADetails