Author/Authors :
Paul S. Humphries، نويسنده , , Jonathon V. Almaden، نويسنده , , Sandra J. Barnum، نويسنده , , Thomas J. Carlson، نويسنده , , Quyen-Quyen T. Do، نويسنده , , James D. Fraser، نويسنده , , Mary Hess، نويسنده , , Young H. Kim، نويسنده , , Kathleen M. Ogilvie، نويسنده , , Shaoxian Sun، نويسنده ,
Abstract :
A series of novel pyridine-2-propanoic acids was synthesized. A structure–activity relationship study of these compounds led to the identification of potent dual PPARα/γ agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compound (S)-13 was selected for further profiling.
Keywords :
PPAR , Diabetes , parallel synthesis , SAR , Pharmacokinetic studies , In vivo efficacy
