Basic Information
ID: ALA1136128
Journal: Bioorg Med Chem Lett
Title: 3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators.
Authors: Sammelson RE, Ma T, Galietta LJ, Verkman AS, Kurth MJ.
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 microM.
CiteXplore: 12852954
DOI: 10.1016/s0960-894x(03)00482-7
Patent ID: ┄
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