3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: Synthesis and evaluation as CFTR activators

Robert E. Sammelson, T. Ma, Luis J V Galietta, A. S. Verkman, Mark J. Kurth

Research output: Contribution to journalArticle

37 Scopus citations

Abstract

A novel class of activators for chloride conductance in the cystic fibrosis transmembrane conductance regulator (CFTR) protein has been identified. These 3-(2-benzyloxyphenyl)isoxazoles and 3-(2-benzyloxyphenyl)isoxazolines were synthesized employing the 1,3-dipolar cycloaddition of nitrile oxides with various alkene and alkyne dipolarophiles. Utilizing a fluorescence cell-based assay of halide transport, the best compounds increased CFTR-dependent chloride transport with half-maximal stimulation at 20-50 μM.

Original languageEnglish (US)
Pages (from-to)2509-2512
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number15
DOIs
StatePublished - Aug 4 2003

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ASJC Scopus subject areas

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

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