Anthranilic acid derivatives as novel ligands for farnesoid X receptor (FXR)

…, O Werz, G Schneider, M Schubert-Zsilavecz

Index: Merk, Daniel; Gabler, Matthias; Gomez, Roberto Carrasco; Flesch, Daniel; Hanke, Thomas; Kaiser, Astrid; Lamers, Christina; Werz, Oliver; Schneider, Gisbert; Schubert-Zsilavecz, Manfred Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 8 p. 2447 - 2460

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Citation Number: 8

Abstract

Abstract Nuclear farnesoid X receptor (FXR) has important physiological roles in various metabolic pathways including bile acid, cholesterol and glucose homeostasis. The clinical use of known synthetic non-steroidal FXR ligands is restricted due to toxicity or poor bioavailability. Here we report the development, synthesis, in vitro activity and structure– activity relationship (SAR) of anthranilic acid derivatives as novel FXR ligands. Starting ...