Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5586-90. doi: 10.1016/j.bmcl.2008.08.112.
Harikishore Pingali  1 ,  Mukul Jain ,  Shailesh Shah ,  Sujay Basu ,  Pankaj Makadia ,  Amitgiri Goswami ,  Pandurang Zaware ,  Pravin Patil ,  Atul Godha ,  Suresh Giri ,  Ashish Goel ,  Megha Patel ,  Harilal Patel ,  Pankaj Patel
Affiliations
  • 1. Zydus Research Centre, Sarkhej-Bavla N.H 8A Moraiya, Ahmedabad 382210, India.
PMID: 18805005 DOI: 10.1016/j.bmcl.2008.08.112
Abstract

A series of novel 1,3-dioxane-2-carboxylic acid derivatives containing alkyl chain tether and substituted phenyl group as a lipophilic tail have been prepared as agonists of PPARalpha and gamma. c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid 13c exhibited potent hypoglycemic and lipid lowering activity with high oral bioavailability in animal models.