O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.
A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARalpha-weighted agonists do not show the typical PPARgamma associated side effects of BAT proliferation and cardiac hypertrophy in a rat tolerability assay.
Adams
Alan D
AD
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co. Inc., PO Box 2000 Rahway, NJ 07065, USA. alan_adams@merck.com
Hu
Zao
Z
von Langen
Derek
D
Dadiz
Adonis
A
Elbrecht
Alex
A
MacNaul
Karen L
KL
Berger
Joel P
JP
Zhou
Gaochao
G
Doebber
Thomas W
TW
Meurer
Roger
R
Forrest
Michael J
MJ
Moller
David E
DE
Jones
A Brian
AB
D000818:Animals; D008333:Mandelic Acids / Q000378:metabolism / Q000494:pharmacology*; D051379:Mice; D008810:Mice, Inbred C57BL; D008822:Mice, Transgenic; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D051381:Rats; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000378:metabolism; D014157:Transcription Factors / Q000819:agonists* / Q000378:metabolism
D008333:Mandelic Acids; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors