(19)F-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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3274619 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2011.12.128 | DOI Listing |
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