1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
A series of highly potent and selective PPARdelta agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 microM, making it a useful tool in studying the biological effects of selective PPARdelta activation.
Epple
Robert
R
Department of Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA. repple@gnf.org
Azimioara
Mihai
M
Russo
Ross
R
Bursulaya
Badry
B
Tian
Shin-Shay
SS
Gerken
Andrea
A
Iskandar
Maya
M
D002087:Butyrates / Q000737:chemistry* / Q000378:metabolism*; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D047494:PPAR delta / Q000819:agonists* / Q000737:chemistry / Q000378:metabolism*; D010671:Phenylurea Compounds / Q000737:chemistry* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D002087:Butyrates; C110636:GW 2433; D008024:Ligands; D047494:PPAR delta; D010671:Phenylurea Compounds