Abstract
19F-modified bithiazole correctors and phenylglycine potentiators of the DF508-CFTR chloride channel were synthesized and their function assayed in cells expressing human DF508-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 DF508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 1602-1605 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 22 |
| Issue number | 4 |
| DOIs | |
| State | Published - Feb 15 2012 |
Keywords
- Corrector
- Cystic fibrosis
- DF508-CFTR
- PET
- Potentiator
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry
- Medicine(all)
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Cite this
Davison, H. R., Solano, D. M., Phuan, P. W., Verkman, A. S., & Kurth, M. J. (2012). Fluorinated DF508-CFTR correctors and potentiators for PET imaging. Bioorganic and Medicinal Chemistry Letters, 22(4), 1602-1605. https://doi.org/10.1016/j.bmcl.2011.12.128