Development of Fibrates as Important Scaffolds in Medicinal Chemistry

Abstract Fibrates are a class of phenoxyisobutyric acid derivatives mainly used as anti‐hyperlipidemic agents. The fibrate scaffold has undergone a variety of chemical modifications, providing a wide spectrum of biological activities. Within the last few years, the majority of new synthetic fibrate derivatives have demonstrated hypolipidemic activity through peroxisome proliferator‐activated receptor α (PPARα) activation. However, some compounds containing the fibrate scaffold have shown different pharmacological properties, also independent of PPARα activation, such as anti‐inflammatory, analgesic, antioxidant, and antiplatelet activities. The aim of this review is to highlight the structure–activity relationships (SAR) in evaluating the significance of fibrates in the field of medicinal chemistry.