2. Academic Validation
  3. Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists

Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists

  • J Med Chem. 2004 May 6;47(10):2422-5. doi: 10.1021/jm0342616.
Yanping Xu 1,  Christopher J Rito,  Garret J Etgen,  Robert J Ardecky,  James S Bean,  William R Bensch,  Jacob R Bosley,  Carol L Broderick,  Dawn A Brooks,  Samuel J Dominianni,  Patric J Hahn,  Sha Liu,  Dale E Mais,  Chahrzad Montrose-Rafizadeh,  Kathy M Ogilvie,  Brian A Oldham,  Mary Peters,  Deepa K Rungta,  Anthony J Shuker,  Gregory A Stephenson,  Allie E Tripp,  Sarah B Wilson,  Leonard L Winneroski,  Richard Zink,  Raymond F Kauffman,  James R McCarthy
Affiliations

Affiliation

  • 1 Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. xu_yanping@lilly.com
PMID: 15115385 DOI: 10.1021/jm0342616
Abstract

The design and synthesis of the dual peroxisome proliferator activated receptor (PPAR) alpha/gamma agonist (S)-2-methyl-3-[4-[2-(5-methyl-2-thiophen-2-yl-oxazol-4-yl)ethoxy]phenyl]-2-phenoxypropionic acid (2) for the treatment of type 2 diabetes and associated dyslipidemia are described. 2 possesses a potent dual hPPAR alpha/gamma agonist profile (IC(50) = 28 and 10 nM; EC(50) = 9 and 4 nM, respectively, for hPPARalpha and hPPARgamma). In preclinical models, 2 substantially improves Insulin sensitivity and potently reverses diabetic hyperglycemia while significantly improving overall lipid homeostasis.

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