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) |
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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)