1350187-64-2Relevant academic research and scientific papers
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate
Boubia, Bena?ssa,Poupardin, Olivia,Barth, Martine,Binet, Jean,Peralba, Philippe,Mounier, Laurent,Jacquier, Elise,Gauthier, Emilie,Lepais, Valérie,Chatar, Maryline,Ferry, Stéphanie,Thourigny, Anne,Guillier, Fabrice,Llacer, Jonathan,Amaudrut, JéRome,Dodey, Pierre,Lacombe, Olivier,Masson, Philippe,Montalbetti, Christian,Wettstein, Guillaume,Luccarini, Jean-Michel,Legendre, Christiane,Junien, Jean-Louis,Broqua, Pierre
, p. 2246 - 2265 (2018/03/26)
Here, we describe the identification and synthesis of novel indole sulfonamide derivatives that activate the three peroxisome proliferator activated receptor (PPAR) isoforms. Starting with a PPARα activator, compound 4, identified during a high throughput screening (HTS) of our proprietary screening library, a systematic optimization led to the discovery of lanifibranor (IVA337) 5, a moderately potent and well balanced pan PPAR agonist with an excellent safety profile. In vitro and in vivo, compound 5 demonstrated strong activity in models that are relevant to nonalcoholic steatohepatitis (NASH) pathophysiology suggesting therapeutic potential for NASH patients.
