Sulfamoyl-4-oxoquinoline-3-carboxamides: Novel potentiators of defective ΔF508-cystic fibrosis transmembrane conductance regulator chloride channel gating

The synthesis of a small collection of sulfamoyl-4-oxoquinoline-3-carboxamides is described for use as correctors of defective gating of the ΔF508-cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. Several compounds with submicromolar potency were obtained. N-Ethyl 6-(ethylphenylsulfamoyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (7b) was found to be the most effective sulfonamide corrector of defective ΔF508-CFTR gating.

Evaluation and synthesis of sulfamoyl-4-oxoquinoline-3-carboxamide correctors of defective gating of the ΔF508-cystic fibrosis transmembrane conductance regulator chloride channel are reported.Figure optionsDownload as PowerPoint slide