Communication

Design and Biological Evaluation of Novel, Balanced Dual PPARα/γ Agonists

  1. Uwe Grether Dr.1,
  2. Agnes Bénardeau Dr.1,
  3. Jörg Benz Dr.1,
  4. Alfred Binggeli1,
  5. Denise Blum1,
  6. Hans Hilpert Dr.1,
  7. Bernd Kuhn Dr.1,
  8. Hans Peter Märki Dr.1,
  9. Markus Meyer Dr.2,
  10. Peter Mohr Dr.1,
  11. Kurt Püntener Dr.1,
  12. Susanne Raab Dr.1,
  13. Armin Ruf Dr.1,
  14. Daniel Schlatter Dr.1

Article first published online: 26 MAR 2009

DOI: 10.1002/cmdc.200800425

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, pages 951–956, June 8, 2009

Additional Information

How to Cite

Grether, U., Bénardeau, A., Benz, J., Binggeli, A., Blum, D., Hilpert, H., Kuhn, B., Märki, H. P., Meyer, M., Mohr, P., Püntener, K., Raab, S., Ruf, A. and Schlatter, D. (2009), Design and Biological Evaluation of Novel, Balanced Dual PPARα/γ Agonists. ChemMedChem, 4: 951–956. doi: 10.1002/cmdc.200800425

Author Information

  1. 1

    Pharma Research, F. Hoffmann-La Roche Ltd., 4070 Basel (Switzerland), Fax: (+41) 61688544

  2. 2

    Pharma Development, F. Hoffmann-La Roche Ltd., 4070 Basel (Switzerland)

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 26 MAR 2009
  3. Manuscript Revised: 9 FEB 2009
  4. Manuscript Received: 11 DEC 2008

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Keywords:

  • aryl propionic acids;
  • drug design;
  • PPAR;
  • receptors;
  • X-ray crystal structures

Abstract

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An X-ray-guided design approach led to the identification of a novel, balanced class of α-ethoxy-phenylpropionic acid-derived dual PPARα/γ agonists. The series shows a wide range of PPARα/γ ratios within a rather narrow structural space. Advanced compounds possess favorable physicochemical and pharmacokinetic profiles and show a high efficacy in T2D and dyslipidemia animal models.

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