Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.
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ABSTRACT:
SUBMITTER: Sepe V
PROVIDER: S-EPMC6466548 | biostudies-literature | 2019 Apr
REPOSITORIES: biostudies-literature
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Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.
Sepe Valentina V Marchianò Silvia S Finamore Claudia C Baronissi Giuliana G Di Leva Francesco Saverio FS Carino Adriana A Biagioli Michele M Fiorucci Chiara C Cassiano Chiara C Monti Maria Chiara MC Del Gaudio Federica F Novellino Ettore E Limongelli Vittorio V Fiorucci Stefano S Zampella Angela A
ACS medicinal chemistry letters 20181206 4
Acetaminophen misuse is a leading cause of acute liver failure and liver transplantation for which therapy is poorly effective. FXR ligands have shown effective in reducing liver injury in several experimental and clinical settings. In this Letter, we have elaborated on the structure of GW4064, the first nonsteroidal agonist for FXR, to identify novel isoxazoles endowed with FXR agonistic activity and improved ADME properties. The pharmacological characterization and molecular docking studies fo ...[more]
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