title: Sulfamoyl-4-oxoquinoline-3-carboxamides: novel potentiators of defective DeltaF508-cystic fibrosis transmembrane conductance regulator chloride channel gating.
abstract: The synthesis of a small collection of sulfamoyl-4-oxoquinoline-3-carboxamides is described for use as correctors of defective gating of the DeltaF508-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 DeltaF508-CFTR gating.
authors.affiliation: Department of Chemistry, University of California, Davis, CA 95616, USA.
authors.forename: Yat Fan
authors.initials: YF
authors.lastname: Suen
authors.forename: Lori
authors.initials: L
authors.lastname: Robins
authors.forename: Baoxue
authors.initials: B
authors.lastname: Yang
authors.forename: A S
authors.initials: AS
authors.lastname: Verkman
authors.forename: Michael H
authors.initials: MH
authors.lastname: Nantz
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Kurth
mesh_terms: D018118:Chloride Channels / Q000378:metabolism*; D019005:Cystic Fibrosis Transmembrane Conductance Regulator / Q000187:drug effects / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects* / Q000502:physiology; D008956:Models, Chemical; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D018118:Chloride Channels; D015363:Quinolones; D013449:Sulfonamides; C093349:cystic fibrosis transmembrane conductance regulator delta F508; D019005:Cystic Fibrosis Transmembrane Conductance Regulator