Hypoglycemic activity of a series of alpha-alkylthio and alpha-alkoxy carboxylic acids related to ciglitazone

J Med Chem. 1996 Sep 27;39(20):3897-907. doi: 10.1021/jm960230h.

Abstract

The thiazolidinedione moiety of ciglitazone and its analogues can be replaced by an alpha-alkoxy or alpha-thioether carboxylic acid group. The influence of the nature of the R group, the length of the connector to the aromatic backbone of the molecule, and the stereochemistry have been studied. The most potent compounds have glucose-lowering activity at doses as low as 0.01 mg/kg.

MeSH terms

  • 3T3 Cells
  • Adipocytes / drug effects
  • Animals
  • Benzofurans / chemistry*
  • Benzofurans / pharmacology
  • Benzofurans / therapeutic use
  • Carboxylic Acids / chemistry*
  • Diabetes Mellitus, Type 2 / drug therapy
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / therapeutic use*
  • Mice
  • Mice, Mutant Strains
  • Mice, Obese
  • Molecular Structure
  • Oxazoles / chemistry*
  • Oxazoles / pharmacology
  • Oxazoles / therapeutic use
  • Stereoisomerism
  • Structure-Activity Relationship
  • Thiazoles / chemistry*
  • Thiazolidinediones*

Substances

  • Benzofurans
  • Carboxylic Acids
  • Hypoglycemic Agents
  • Oxazoles
  • Thiazoles
  • Thiazolidinediones
  • 2-ethoxy-3-(2-((5-methyl-2-phenyloxazol-4-yl)methyl)benzofuran-5-yl)propionic acid
  • 3-(2-((5-methyl-2-phenyloxazol-4-yl)methyl)benzofuran-5-yl)-2-(propylsulfanyl)propionic acid
  • ciglitazone