Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation

We have succeeded in synthesizing a novel PPARδ selective agonist, compound 20, characterized by a benzisoxazole ring. Compound 20 exhibited a potent hPPARδ transactivation activity and high δ selectivity. Compound 20 stimulated oligodendrocyte differentiation of primary oligodendrocyte precursors c...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.240-244
Hauptverfasser: Sakuma, Shogo, Endo, Tsuyoshi, Kanda, Takashi, Nakamura, Hideki, Yamasaki, Satomi, Yamakawa, Tomio
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Sprache:eng
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Zusammenfassung:We have succeeded in synthesizing a novel PPARδ selective agonist, compound 20, characterized by a benzisoxazole ring. Compound 20 exhibited a potent hPPARδ transactivation activity and high δ selectivity. Compound 20 stimulated oligodendrocyte differentiation of primary oligodendrocyte precursors cells in vitro, indicating that it may be an effective drug to treat demyelinating disorders, such as multiple sclerosis. We successfully synthesized a novel peroxisome proliferator-activated receptor (PPAR)δ selective agonist, namely, compound 20, with a characteristic benzisoxazole ring. Compound 20 exhibited potent human PPARδ transactivation activity and high δ selectivity. Further, it stimulated differentiation of primary oligodendrocyte precursor cells in vitro, indicating that it may be an effective drug in the treatment of demyelinating disorders such as multiple sclerosis.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.11.030