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Abstract #1991

Pentafluorosulfanyl (SF5) is a Superior 19F Magnetic Resonance Reporter Group: Signal Detection of Teriflunomide Derivatives

Ashrith Jacob1, Ludger Starke1, Christian Prinz1, Jason M Millward1, Paula Ramos Delgado1, Ariane Fillmer2, Thoralf Niendorf1, and Sonia Waiczies1
1Berlin Ultrahigh Field Facility, MDC, Berlin, Germany, 2Physikalisch - Technische Bundesanstalt (PTB) Braunschweig and Berlin, Berlin, Germany


Modifications to the CF3 side-group of teriflunomide were made to improve its detection by 19F MRI. Pentafluorosulfanyl (SF5) was shown to be a superior alternative to CF3. The SNR efficiency of three 19F MRI methods showed that within a biological environment, SF5-substitutions gave the highest SNR efficiency in combination with an ultrashort echo-time (UTE) MRI method. Chemical modifications did not hamper biological activity but SF5-TF was more effective to inhibit T cell proliferation, indicating better anti-inflammatory activity. This study proposes SF5 as a novel superior 19F MR reporter group for the drug teriflunomide.

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