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

@article{Sammelson200332BenzyloxyphenylisoxazolesAI,
  title={3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators.},
  author={Robert E Sammelson and Teng Ma and Luis J. V. Galietta and Alan S. Verkman and Mark J Kurth},
  journal={Bioorganic & medicinal chemistry letters},
  year={2003},
  volume={13 15},
  pages={2509-12}
}
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… CONTINUE READING

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