2-(Dialkylamino)-4H-1-benzopyran-4-one derivatives modify chloride conductance in CFTR expressing cells

Mauro Mazzei, Erika Nieddu, Chiara Folli, Emanuela Caci, Louis V J Galietta

Research output: Contribution to journalArticlepeer-review

Abstract

Some 2-(diethylamino)-7-hydroxy-4H-1-benzopyran-4-one derivatives, potentially useful as activators of the cystic fibrosis transmembrane conductance regulator (CFTR), were prepared. The synthesized compounds were tested, together with others 2-(dialkylamino)-7-hydroxybenzopyran-4-one derivatives, by measuring their capacity to modify the kinetics of iodide influx in Fisher rat thyroid cells expressing wild type CFTR and the halide-sensitive yellow fluorescent protein. Among the tested compounds the dinitrile derivatives 8 and 9 are endowed with an activity comparable to the reference compound apigenin.

Original languageEnglish
Pages (from-to)961-970
Number of pages10
JournalFarmaco
Volume58
Issue number9
DOIs
Publication statusPublished - Sep 1 2003

Keywords

  • Benzopyran-4-one derivatives
  • CFTR
  • Cystic fibrosis

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmaceutical Science

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