Heteroaryl substituted bis-trifluoromethyl carbinols as malonyl-CoA decarboxylase inhibitors

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3484-8. doi: 10.1016/j.bmcl.2006.03.100. Epub 2006 Apr 27.

Abstract

A series of heteroaryl-substituted bis-trifluoromethyl carbinols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some thiazole-based derivatives showed potent in vitro MCD inhibitory activities and significantly increased glucose oxidation rates in isolated working rat hearts.

MeSH terms

  • Animals
  • Carboxy-Lyases / antagonists & inhibitors*
  • Drug Evaluation, Preclinical
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Glucose / chemistry
  • Glucose / metabolism
  • Heart / drug effects
  • Heterocyclic Compounds / chemistry*
  • In Vitro Techniques
  • Methanol / analogs & derivatives
  • Methanol / chemical synthesis*
  • Methanol / pharmacology*
  • Molecular Structure
  • Oxidation-Reduction
  • Rats
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Heterocyclic Compounds
  • Carboxy-Lyases
  • malonyl-CoA decarboxylase
  • Glucose
  • Methanol