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.

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Pingali H, Jain M, Shah S, Basu S, Makadia P, Goswami A, Zaware P, Patil P, Godha A, Giri S, Goel A, Patel M, Patel H, Patel P

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. Epub 2008 Sep 3.

PubMed ID

18805005 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tesaglitazar	Peroxisome proliferator-activated receptor alpha	EC 50 (nM)	820	N/A	N/A	Details
Tesaglitazar	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	13	N/A	N/A	Details