Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta

K G Liu; J S Smith; A H Ayscue; B R Henke; M H Lambert; L M Leesnitzer; K D Plunket; T M Willson; D D Sternbach

doi:10.1016/s0960-894x(01)00458-9

Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2385-8. doi: 10.1016/s0960-894x(01)00458-9.

Authors

K G Liu¹, J S Smith, A H Ayscue, B R Henke, M H Lambert, L M Leesnitzer, K D Plunket, T M Willson, D D Sternbach

Affiliation

¹ Nuclear Receptor Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. kevin_liu@stromix.com

PMID: 11527737
DOI: 10.1016/s0960-894x(01)00458-9

Abstract

A series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with dual agonist activity on PPARalpha and PPARgamma is described. Several of these compounds also showed partial agonist activity on PPARdelta. Resolution of one analogue showed that PPARalpha and PPARgamma activity resided in mainly one enantiomer, whereas PPARdelta activity was retained in both enantiomers.

MeSH terms

Chromatography, High Pressure Liquid
Drug Design
Drug Evaluation, Preclinical
Humans
Isomerism
Oxadiazoles / chemistry
Receptors, Cytoplasmic and Nuclear / agonists*
Structure-Activity Relationship
Transcription Factors / agonists*

Substances

Oxadiazoles
Receptors, Cytoplasmic and Nuclear
Transcription Factors