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
  • 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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