Biological evaluation of novel benzisoxazole derivatives as PPAR[delta] agonists

We discovered novel peroxisome proliferator-activated receptor [delta] agonists with a characteristic benzisoxazole ring. Compound 5 exhibited potent human PPAR[delta] transactivation activity. Furthermore, it stimulated the differentiation of oligodendrocyte precursor cells in vitro. This indicates...

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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
Format: Artikel
Sprache:eng
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Zusammenfassung:We discovered novel peroxisome proliferator-activated receptor [delta] agonists with a characteristic benzisoxazole ring. Compound 5 exhibited potent human PPAR[delta] 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
DOI:10.1016/j.bmc.2011.03.053