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Discovery of *Trypanosoma brucei* inhibitors enabled by a unified synthesis of diverse sulfonyl fluorides

Chemistry

Discovery of *Trypanosoma brucei* inhibitors enabled by a unified synthesis of diverse sulfonyl fluorides

B. S. Mantilla, J. S. White, et al.

Discover the groundbreaking research conducted by Brian S. Mantilla and colleagues at the University of Leeds and the University of St Andrews, who developed a unified synthesis of sulfonyl fluorides. Their innovative photoredox-catalyzed approach led to the identification of compounds with remarkable anti-trypanosomal activity, revealing new therapeutic potential against *Trypanosoma brucei*.

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~3 min • Beginner • English
Abstract
A unified synthesis of skeletally-diverse sulfonyl fluorides was developed using photoredox-catalysed dehydrogenative couplings between hetaryl sulfonyl fluorides and hydrogen donor building blocks. A set of 32 diverse electrophilic probes was prepared and screened against Trypanosoma brucei; four probes showed sub-micromolar activity. An alkynylated analogue and broad-spectrum fluorophosphonate tools enabled chemical proteomic studies that suggest anti-trypanosomal activity arises from covalent modification of multiple protein targets. This unified diversity-oriented approach may facilitate discovery of electrophilic probes valuable for elucidating biological mechanisms.
Publisher
Communications Chemistry
Published On
Oct 19, 2024
Authors
Brian S. Mantilla, Jack S. White, William R. T. Mosedale, Andrew Gomm, Adam Nelson, Terry K. Smith, Megan H. Wright
DOI
https://doi.org/https://doi.org/10.1038/s42004-024-01327-8
Tags
sulfonyl fluorides
photoredox-catalyzed
anti-trypanosomal
chemical proteomics
dehydrogenative couplings
Trypanosoma brucei
covalent modification

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