title: 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.
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.
authors.affiliation: Zydus Research Centre, Sarkhej-Bavla N.H 8A Moraiya, Ahmedabad 382210, India.
authors.forename: Harikishore
authors.initials: H
authors.lastname: Pingali
authors.forename: Mukul
authors.initials: M
authors.lastname: Jain
authors.forename: Shailesh
authors.initials: S
authors.lastname: Shah
authors.forename: Sujay
authors.initials: S
authors.lastname: Basu
authors.forename: Pankaj
authors.initials: P
authors.lastname: Makadia
authors.forename: Amitgiri
authors.initials: A
authors.lastname: Goswami
authors.forename: Pandurang
authors.initials: P
authors.lastname: Zaware
authors.forename: Pravin
authors.initials: P
authors.lastname: Patil
authors.forename: Atul
authors.initials: A
authors.lastname: Godha
authors.forename: Suresh
authors.initials: S
authors.lastname: Giri
authors.forename: Ashish
authors.initials: A
authors.lastname: Goel
authors.forename: Megha
authors.initials: M
authors.lastname: Patel
authors.forename: Harilal
authors.initials: H
authors.lastname: Patel
authors.forename: Pankaj
authors.initials: P
authors.lastname: Patel
mesh_terms: D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004146:Dioxanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis*; D008055:Lipids / Q000737:chemistry; D008698:Mesylates / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051379:Mice; D008956:Models, Chemical; D047493:PPAR alpha / Q000378:metabolism; D047495:PPAR gamma / Q000378:metabolism; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists; D051381:Rats; D017208:Rats, Wistar; D015533:Transcriptional Activation
chemical_list: C540066:5-(6-(4-methanesulfonyloxyphenyl)hexyl)-2-methyl-1,3-dioxane-2-carboxylic acid; D002264:Carboxylic Acids; D004146:Dioxanes; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D008055:Lipids; D008698:Mesylates; D047493:PPAR alpha; D047495:PPAR gamma; D047492:Peroxisome Proliferator-Activated Receptors