2. Academic Validation
  3. Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists

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

Affiliation

  • 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.

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