Author/Authors :
Wei Wang، نويسنده , , Pratik Devasthale، نويسنده , , Dennis Farrelly، نويسنده , , Liqun Gu، نويسنده , , Thomas Harrity، نويسنده , , Michael Cap، نويسنده , , Cuixia Chu، نويسنده , , Lori Kunselman، نويسنده , , Nathan Morgan، نويسنده , , Randy Ponticiello، نويسنده , , Rachel Zebo، نويسنده , , Litao Zhang، نويسنده , , Kenneth Locke، نويسنده , , Jonathan Lippy، نويسنده , , Kevin O’Malley، نويسنده , , Vinayak Hosagrahara، نويسنده , , Lisa Zhang، نويسنده , , Pathanjali Kadiyala، نويسنده , , Chiehying Chang، نويسنده , , Jodi Muckelbauer، نويسنده , , et al.، نويسنده ,
Abstract :
A novel class of azetidinone acid-derived dual PPARα/γ agonists has been synthesized for the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for binding and functional agonist activity against both PPARα and PPARγ receptors was shown to be 3S,4S. Synthesis, in vitro and in vivo activities of compounds in this series are described. A high-yielding method for N-arylation of azetidinone esters is also described.
Keywords :
Dual PPAR?/? agonists , Antidiabetic azetidinones , PPAR , conformational constraint , Boronic acid coupling
