Literature DB >> 30957432

Development of Fibrates as Important Scaffolds in Medicinal Chemistry.

Letizia Giampietro1, Alessandra Ammazzalorso1, Rosa Amoroso1, Barbara De Filippis1.   

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.
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  PPARs; fibrates; hybrids; hypolipidemic agents; phenoxypropanoic acid

Mesh:

Substances:

Year:  2019        PMID: 30957432     DOI: 10.1002/cmdc.201900128

Source DB:  PubMed          Journal:  ChemMedChem        ISSN: 1860-7179            Impact factor:   3.466


  6 in total

1.  Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study.

Authors:  Pasquale Linciano; Barbara De Filippis; Alessandra Ammazzalorso; Pasquale Amoia; Felisa Cilurzo; Marialuigia Fantacuzzi; Letizia Giampietro; Cristina Maccallini; Charlotte Petit; Rosa Amoroso
Journal:  Medchemcomm       Date:  2019-08-15       Impact factor: 3.597

2.  Juice from Fructus Rosae Roxburghii normalizes blood lipids in mice with diet-induced hyperlipidemia*.

Authors:  Pingping Song; Xiangchun Shen
Journal:  Food Sci Nutr       Date:  2020-09-18       Impact factor: 2.863

3.  Structural Analysis of Human Serum Albumin in Complex with the Fibrate Drug Gemfibrozil.

Authors:  Stefano Liberi; Sara Linciano; Giulia Moro; Luca De Toni; Laura Cendron; Alessandro Angelini
Journal:  Int J Mol Sci       Date:  2022-02-04       Impact factor: 5.923

4.  The Small Molecule PPARγ Agonist GL516 Induces Feeding-Stimulatory Effects in Hypothalamus Cells Hypo-E22 and Isolated Hypothalami.

Authors:  Annalisa Chiavaroli; Viviana di Giacomo; Barbara De Filippis; Amelia Cataldi; Claudio Ferrante; Letizia Giampietro
Journal:  Molecules       Date:  2022-07-30       Impact factor: 4.927

5.  Fenofibrate and Impaired Taste Perception in Type 2 Diabetes.

Authors:  Timothy M E Davis
Journal:  Am J Case Rep       Date:  2020-11-20

6.  Synthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPARγ Modulators: An In Combo Study.

Authors:  Blanca Colin-Lozano; Héctor Torres-Gomez; Sergio Hidalgo-Figueroa; Fabiola Chávez-Silva; Samuel Estrada-Soto; Julio Cesar Almanza-Pérez; Gabriel Navarrete-Vazquez
Journal:  Pharmaceuticals (Basel)       Date:  2022-01-15
  6 in total

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