2. Academic Validation
  3. Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists

Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists

  • Bioorg Med Chem Lett. 2007 Aug 15;17(16):4689-93. doi: 10.1016/j.bmcl.2007.05.066.
Yukiyoshi Yamazaki 1,  Kazutoyo Abe,  Tsutomu Toma,  Masahiro Nishikawa,  Hidefumi Ozawa,  Ayumu Okuda,  Takaaki Araki,  Soichi Oda,  Keisuke Inoue,  Kimiyuki Shibuya,  Bart Staels,  Jean-Charles Fruchart
Affiliations

Affiliation

  • 1 Tokyo New Drug Research Laboratories 1, Pharmaceutical Division, Kowa Co., LTD, 2-17-43, Noguchicho, Higashimurayam, Tokyo 189-0022, Japan. [email protected]
PMID: 17553678 DOI: 10.1016/j.bmcl.2007.05.066
Abstract

A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human Peroxisome Proliferator-activated Receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.

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