Abstract
Molecular pharmacological evidence that metabolic nuclear receptor peroxisome proliferator-activated receptors (PPARs) act as master regulators of lipid, lipoprotein and glucose homeostasis, in combination with the timely identification of fibrates and glitazones as selective PPARα and PPARγ agonists, and the rapid development of the parallel high-throughput screening (HTS) methods to evaluate activity towards PPAR subtypes (PPARα, PPARδ and PPARγ), has provided an opportunity to develop novel subtype-selective PPAR ligands. This review summarises patent applications disclosing medicinal-chemical strategies to identify new PPAR ligands during 2004. The historical development of PPAR ligands is also reviewed briefly to help to understand the detailed structure–activity relationships (SAR) and the interaction between ligands and PPARs. Current developments are expected to lead to novel therapeutic choices for the treatment of altered metabolic homeostasis, such as dyslipidaemia, diabetes and obesity.
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