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Bioorg Med Chem Lett. 2008 Sep 15;18(18):5018-22. doi: 10.1016/j.bmcl.2008.08.011. Epub 2008 Aug 9.

Discovery of a novel class of PPARdelta partial agonists.

Author information

1
Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA. barry.g.shearer@gsk.com

Abstract

Anthranilic acid GW9371 was identified as a novel class of PPARdelta partial agonist through high-throughput screening. The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells.

PMID:
18722772
DOI:
10.1016/j.bmcl.2008.08.011
[Indexed for MEDLINE]

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