Van der Plas, Steven E.; Kelgtermans, Hans; Mammoliti, Oscar; Menet, Christel; Tricarico, Giovanni; De Blieck, Ann; Joannesse, Caroline; De Munck, Tom; Lambin, Dominique; Cowart, Marlon; Dropsit, Sebastien; Martina, Sebastien L. X.; Gees, Maarten; Wesse, Anne-Sophie; Conrath, Katja; Andrews, Martin published the artcile< Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis>, Formula: C6H5BrN2O2, the main research area is preparation GLPG2451 analog CFTR potentiator cystic fibrosis structure.
Cystic fibrosis (CF) is a life-threatening recessive genetic disease caused by mutations in the gene encoding for the cystic fibrosis transmembrane conductance regulator (CFTR). With the discovery of Ivacaftor and Lumacaftor, it has been shown that administration of one or more small mols. can partially restore the CFTR function. Correctors are small mols. that enhance the amount of CFTR on the cell surface, while potentiators improve the gating function of the CFTR channel. Herein, the discovery and optimization of a novel potentiator series are described. Scaffold hopping, focusing on retaining the different intramol. contacts, was crucial in the whole discovery process to identify a novel series devoid of genotoxic liabilities. From this series, the clin. candidate GLPG2451 was selected based on its pharmacokinetic properties, allowing QD dosing and based on its low CYP induction potential.
Journal of Medicinal Chemistry published new progress about CFTR (cystic fibrosis transmembrane conductance regulator) Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Formula: C6H5BrN2O2.