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

Yat Fan Suen, Lori Robins, Baoxue Yang, A. S. Verkman, Michael H. Nantz, Mark J. Kurth

Research output: Contribution to journalArticle

23 Citations (Scopus)

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 ΔF508-CFTR gating.

Original languageEnglish (US)
Pages (from-to)537-540
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number3
DOIs
StatePublished - Feb 1 2006

Fingerprint

4-Quinolones
Cystic Fibrosis Transmembrane Conductance Regulator
Chloride Channels
Sulfonamides

Keywords

  • Activator
  • CFTR
  • Cystic fibrosis
  • Potentiator
  • Sulfonamide

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Sulfamoyl-4-oxoquinoline-3-carboxamides : Novel potentiators of defective ΔF508-cystic fibrosis transmembrane conductance regulator chloride channel gating. / Suen, Yat Fan; Robins, Lori; Yang, Baoxue; Verkman, A. S.; Nantz, Michael H.; Kurth, Mark J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 3, 01.02.2006, p. 537-540.

Research output: Contribution to journalArticle

Suen, Yat Fan ; Robins, Lori ; Yang, Baoxue ; Verkman, A. S. ; Nantz, Michael H. ; Kurth, Mark J. / Sulfamoyl-4-oxoquinoline-3-carboxamides : Novel potentiators of defective ΔF508-cystic fibrosis transmembrane conductance regulator chloride channel gating. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 3. pp. 537-540.
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