Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6293-7. doi: 10.1016/j.bmcl.2006.09.028. Epub 2006 Sep 26.

Abstract

Novel tetrahydroisoquinolines have been developed as potent PPAR ligands. Evaluation of these compounds in PPARgamma responsive models of type 2 diabetes is described.

MeSH terms

  • Animals
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Humans
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / pharmacology*
  • Mice
  • Models, Molecular
  • PPAR gamma / agonists*
  • PPAR gamma / drug effects
  • Peroxisome Proliferator-Activated Receptors / antagonists & inhibitors
  • Rosiglitazone
  • Tetrahydroisoquinolines / chemistry
  • Tetrahydroisoquinolines / pharmacokinetics
  • Tetrahydroisoquinolines / pharmacology*
  • Thiazolidinediones / pharmacology

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • PPAR gamma
  • Peroxisome Proliferator-Activated Receptors
  • Tetrahydroisoquinolines
  • Thiazolidinediones
  • Rosiglitazone