Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.

Bioorganic & Medicinal Chemistry Letters(2012)

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摘要
19F-modified bithiazole correctors and phenylglycine potentiators of the ΔF508-CFTR chloride channel were synthesized and their function assayed in cells expressing human ΔF508-CFTR and a halide-sensitive fluorescent protein. Fluorine was incorporated into each scaffold using prosthetic groups for future biodistribution imaging studies using positron emission tomography (PET). The ΔF508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.
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关键词
Cystic fibrosis,PET,Corrector,Potentiator,ΔF508-CFTR
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