Pentafluorosulfanyl (SF₅) as a Superior ¹⁹F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives.

ABSTRACT: Fluorine (¹⁹F) magnetic resonance imaging (MRI) is severely limited by a low signal-to noise ratio (SNR), and tapping it for ¹⁹F drug detection in vivo still poses a significant challenge. However, it bears the potential for label-free theranostic imaging. Recently, we detected the fluorinated dihydroorotate dehydrogenase (DHODH) inhibitor teriflunomide (TF) noninvasively in an animal model of multiple sclerosis (MS) using ¹⁹F MR spectroscopy (MRS). In the present study, we probed distinct modifications to the CF₃ group of TF to improve its SNR. This revealed SF₅ as a superior alternative to the CF₃ group. The value of the SF₅ bioisostere as a ¹⁹F MRI reporter group within a biological or pharmacologica

SUBMITTER: Prinz C 

PROVIDER: S-EPMC8630787 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature