Synthetic ligands for PPARγ - review of patent literature 1994 - 1999

Abstract

The recent identification of the nuclear receptor peroxisome proliferator activated receptor-γ (PPARγ) as a primary molecular target for the thiazolidine-2,4-dione (glitazone) class of antihyperglycaemic agents now used in the treatment of Type 2 diabetes has provided an opportunity to develop novel PPARγ pharmacophores. This review outlines the molecular pharmacology of the PPAR family of nuclear receptors and summarises recent patents disclosing medicinal chemistry strategies to identify new PPARγ agonists. We also critically evaluate complementary parallel approaches that target other PPAR subtypes. This may yield useful treatment for other metabolic disorders that, like Type 2 diabetes, are also characterised by an excess cardiovascular risk.

• insulin sensitisers
• peroxisome proliferator activated receptor gamma
• thiazolidine-2,4-dione
• Type 2 diabetes