Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2497-502. doi: 10.1016/j.bmcl.2012.02.006. Epub 2012 Feb 15.

Abstract

A novel class of DGAT1 inhibitors containing a thiadiazole core has been discovered. Chemical optimization lead to inhibitors of human DGAT1 with an appropriate ADME profile and that show in vivo activity in target tissues.

MeSH terms

  • Caco-2 Cells
  • Clinical Trials as Topic
  • Diacylglycerol O-Acyltransferase / antagonists & inhibitors*
  • Diacylglycerol O-Acyltransferase / metabolism
  • Drug Discovery
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / pharmacology
  • Models, Molecular
  • Stereoisomerism
  • Structure-Activity Relationship
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / pharmacology
  • Triglycerides / antagonists & inhibitors*
  • Triglycerides / biosynthesis

Substances

  • Enzyme Inhibitors
  • Hypoglycemic Agents
  • Thiadiazoles
  • Triglycerides
  • DGAT1 protein, human
  • Diacylglycerol O-Acyltransferase