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

…, L Robins, B Yang, AS Verkman, MH Nantz…

Index: Suen, Yat Fan; Robins, Lori; Yang, Baoxue; Verkman; Nantz, Michael H.; Kurth, Mark J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 3 p. 537 - 540

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Citation Number: 28

Abstract

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 ...