Download MendeleyPhenoxyacetic acid PPARd partial agonists for the treatment of type 2 diabetes: synthesis, optimization, and in vivo efficacy
Evans, K.A., Shearer, B.G., Wisnoski, D.D., Shi, D., Sparks, S.M., Sternbach, D.D., Winegar, D.A., Billin, A.N., Britt, C., Way, J.M., Epperly, A.H., Leesnitzer, L.M., Merrihew, R.V., Xu, R.X., Lambert, M.H., Jin, J.(2011) Bioorg Med Chem Lett 21: 2345-2350
- PubMed: 21414782
- DOI: https://doi.org/10.1016/j.bmcl.2011.02.077
- Primary Citation of Related Structures:
3PEQ - PubMed Abstract:
A series of phenoxyacetic acids as subtype selective and potent hPPARδ partial agonists is described. Many analogues were readily accessible via a single solution-phase synthetic route which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of two potent exemplars which were further evaluated in vivo. Details of the SAR, optimization, and in vivo efficacy of this series are presented herein.
Organizational Affiliation:
Discovery Medicinal Chemistry, Discovery Research, GlaxoSmithKline Pharmaceuticals, 1250 South Collegeville Road, PO Box 5089, Collegeville, PA 19426-0989, United States. [email protected]
