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Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists |
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| Authors: | Wang Wei Devasthale Pratik Farrelly Dennis Gu Liqun Harrity Thomas Cap Michael Chu Cuixia Kunselman Lori Morgan Nathan Ponticiello Randy Zebo Rachel Zhang Litao Locke Kenneth Lippy Jonathan O'Malley Kevin Hosagrahara Vinayak Zhang Lisa Kadiyala Pathanjali Chang Chiehying Muckelbauer Jodi Doweyko Arthur M Zahler Robert Ryono Denis Hariharan Narayanan Cheng Peter T W |
| Institution: | Metabolic Diseases Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, USA. |
| Abstract: | A novel class of azetidinone acid-derived dual PPARalpha/gamma 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 PPARalpha and PPARgamma 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. |
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