Development of Fibrates as Important Scaffolds in Medicinal Chemistry

被引：22
作者：
Giampietro, Letizia [1 ]
Ammazzalorso, Alessandra [1 ]
Amoroso, Rosa [1 ]
De Filippis, Barbara [1 ]
机构：
[1] Univ G dAnnunzio, Dipartimento Farm, Via Vestini, I-66100 Chieti, Italy
来源：
CHEMMEDCHEM | 2019年 / 14卷 / 11期
关键词：
fibrates; hybrids; hypolipidemic agents; phenoxypropanoic acid; PPARs; PROLIFERATOR-ACTIVATED RECEPTORS; ALPHA/DELTA AGONIST GFT505; HMG-COA REDUCTASE; PPAR-ALPHA; HYPOLIPIDEMIC ACTIVITY; BIOLOGICAL EVALUATION; ACID-DERIVATIVES; CLOFIBRIC ACID; DUAL AGONISTS; IN-VIVO;
D O I：
10.1002/cmdc.201900128
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 alpha (PPAR alpha) activation. However, some compounds containing the fibrate scaffold have shown different pharmacological properties, also independent of PPAR alpha 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.
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收藏
页码：1051 / 1066
页数：16
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