Synthesis and antidiabetic activity of morpholinothiazolyl-2,4-thiazolidindione derivatives

J Enzyme Inhib Med Chem. 2012 Jun;27(3):419-27. doi: 10.3109/14756366.2011.594047. Epub 2011 Jul 8.

Abstract

We report the synthesis and the in vitro insulin releasing and glucose uptake activity of the morpholino thiazolyl-2,4-thiazolidinediones (1-15). Compounds 5, 11-15 (at lower concentration; 0.001 mg/ml) were able to increase insulin release in the presence of 5.6 mmol/l glucose. The compounds, except derivative 3 show an increase of glucose uptake. Various compounds are interesting potential antidiabetic leads showing pancreatic and extrapancreatic effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Glucose / metabolism
  • Hep G2 Cells
  • Humans
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Insulin / metabolism
  • Insulin Secretion
  • Models, Molecular
  • Molecular Structure
  • Rats
  • Structure-Activity Relationship
  • Thiazolidinediones / chemical synthesis*
  • Thiazolidinediones / chemistry
  • Thiazolidinediones / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Hypoglycemic Agents
  • Insulin
  • Thiazolidinediones
  • Glucose