Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4351-7. doi: 10.1016/j.bmcl.2007.05.017.
Hiroki Fujieda  1 ,  Shinya Usui ,  Takayoshi Suzuki ,  Hidehiko Nakagawa ,  Michitaka Ogura ,  Makoto Makishima ,  Naoki Miyata
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
PMID: 17524643 DOI: 10.1016/j.bmcl.2007.05.017
Abstract

To find novel PPARdelta-selective agonists, we designed and synthesized phenylpropanoic acid derivatives bearing 6-substituted benzothiazoles. Optimization of this series led to the identification of a potent and selective PPARdelta agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARdelta appropriately.