Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists

Oligodendrocyte differentiation-stimulating effect of compound 5. We discovered novel peroxisome proliferator-activated receptor δ agonists with a characteristic benzisoxazole ring. Compound 5 exhibited potent human PPARδ transactivation activity. Furthermore, it stimulated the differentiation of ol...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2011-05, Vol.19 (10), p.3255-3264
Hauptverfasser: Sakuma, Shogo, Endo, Tsuyoshi, Kanda, Takashi, Nakamura, Hideki, Yamasaki, Satomi, Yamakawa, Tomio
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Sprache:eng
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Zusammenfassung:Oligodendrocyte differentiation-stimulating effect of compound 5. We discovered novel peroxisome proliferator-activated receptor δ agonists with a characteristic benzisoxazole ring. Compound 5 exhibited potent human PPARδ 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2011.03.053