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Development of Fibrates as Important Scaffolds in Medicinal Chemistry
Author(s) -
Giampietro Letizia,
Ammazzalorso Alessandra,
Amoroso Rosa,
De Filippis Barbara
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900128
Subject(s) - fibrate , chemistry , peroxisome proliferator activated receptor , scaffold , pharmacology , receptor , biochemistry , statin , biology , medicine , biomedical engineering
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.