Literature DB >> 23102891

Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.

Letizia Giampietro1, Alessandra D'Angelo, Antonella Giancristofaro, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Pasquale Linciano, Cristina Maccallini, Rosa Amoroso.   

Abstract

In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and lipophilic groups derived from natural products chalcone and stilbene were synthesised. Some of them were found to be active at micromolar concentrations only on PPARα or PPARγ, while others were identified as dual agonists PPARα/γ.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23102891     DOI: 10.1016/j.bmcl.2012.09.111

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Novel Phenyldiazenyl Fibrate Analogues as PPAR α/γ/δ Pan-Agonists for the Amelioration of Metabolic Syndrome.

Authors:  Letizia Giampietro; Antonio Laghezza; Carmen Cerchia; Rosalba Florio; Lucia Recinella; Fabio Capone; Alessandra Ammazzalorso; Isabella Bruno; Barbara De Filippis; Marialuigia Fantacuzzi; Claudio Ferrante; Cristina Maccallini; Paolo Tortorella; Fabio Verginelli; Luigi Brunetti; Alessandro Cama; Rosa Amoroso; Fulvio Loiodice; Antonio Lavecchia
Journal:  ACS Med Chem Lett       Date:  2019-02-25       Impact factor: 4.345

2.  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

Review 3.  Deciphering the Roles of Thiazolidinediones and PPARγ in Bladder Cancer.

Authors:  Melody Chiu; Lucien McBeth; Puneet Sindhwani; Terry D Hinds
Journal:  PPAR Res       Date:  2017-02-28       Impact factor: 4.964

4.  Sulfonimide and Amide Derivatives as Novel PPARα Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies.

Authors:  Alessandra Ammazzalorso; Isabella Bruno; Rosalba Florio; Laura De Lellis; Antonio Laghezza; Carmen Cerchia; Barbara De Filippis; Marialuigia Fantacuzzi; Letizia Giampietro; Cristina Maccallini; Paolo Tortorella; Serena Veschi; Fulvio Loiodice; Antonio Lavecchia; Alessandro Cama; Rosa Amoroso
Journal:  ACS Med Chem Lett       Date:  2020-03-03       Impact factor: 4.345

5.  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

6.  Structural Basis for PPARα Activation by 1H-pyrazolo-[3,4-b]pyridine Derivatives.

Authors:  Takuya Yoshida; Hiroya Oki; Michihiro Doi; Syohei Fukuda; Tomohiro Yuzuriha; Ryotaro Tabata; Kenji Ishimoto; Kazuki Kawahara; Tadayasu Ohkubo; Hiroyuki Miyachi; Takefumi Doi; Keisuke Tachibana
Journal:  Sci Rep       Date:  2020-05-06       Impact factor: 4.379

  6 in total

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