TY - JOUR
T1 - 3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines
T2 - Synthesis and evaluation as CFTR activators
AU - Sammelson, Robert E.
AU - Ma, T.
AU - Galietta, Luis J V
AU - Verkman, A. S.
AU - Kurth, Mark J.
PY - 2003/8/4
Y1 - 2003/8/4
N2 - 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.
AB - 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.
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U2 - 10.1016/S0960-894X(03)00482-7
DO - 10.1016/S0960-894X(03)00482-7
M3 - Article
C2 - 12852954
AN - SCOPUS:0037971989
VL - 13
SP - 2509
EP - 2512
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 15
ER -