Title of article :
Design, synthesis, and structure–activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARα/γ agonists
Author/Authors :
Xiang-Yang Ye، نويسنده , , Yi-Xin Li، نويسنده , , Dennis Farrelly، نويسنده , , Neil Flynn، نويسنده , , Liqun Gu، نويسنده , , Kenneth T. Locke، نويسنده , , Jonathan Lippy، نويسنده , , Kevin O’Malley، نويسنده , , Celeste Twamley، نويسنده , , Litao Zhang، نويسنده , , Denis E. Ryono، نويسنده , , Robert Zahler، نويسنده , , Narayanan Hariharan، نويسنده , , Peter T.W. Cheng، نويسنده ,
Abstract :
Several series of substituted dehydropiperidine and piperidine-4-carboxylic acid analogs have been designed and synthesized as novel, potent dual PPARα/γ agonists. The SAR of these series of analogs is discussed. A rare double bond migration occurred during the basic hydrolysis of the α,β-unsaturated dehydropiperidine esters 12, and the structures of the migration products were confirmed through a series of 2D NMR experiments.
Keywords :
Structure–activity relationships , Piperidine and dehydropiperidine carboxylic acids , Dual agonists , Peroxisome proliferator-activated receptors
