2. Academic Validation
  3. Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation

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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):240-4. doi: 10.1016/j.bmcl.2010.11.030.
Shogo Sakuma 1,  Tsuyoshi Endo,  Takashi Kanda,  Hideki Nakamura,  Satomi Yamasaki,  Tomio Yamakawa
Affiliations

Affiliation

  • 1 Discovery Research Laboratories, Nippon Chemiphar Co Ltd, 1-22, Hikokawado, Misato, Saitama 341-0005, Japan. s-sakuma@chemiphar.co.jp
PMID: 21112784 DOI: 10.1016/j.bmcl.2010.11.030
Abstract

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.

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