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I03-Macromolecular Crystallography	Expanding the repertoire of low-molecular-weight pentafluorosulfanyl-substituted scaffolds Arathy Jose , Daniel Guest , Remi Legay , Graham J. Tizzard , Simon Coles , Mariliza Derveni , Edward Wright , Lester Marrison , Alpha A. Lee , Aaron Morris , Matt Robinson , Frank Von Delft , Daren Fearon , Lizbe Koekemoer , Tetiana Matviuk , Anthony Aimon , Christopher J. Schofield , Tika R. Malla , Nir London , Barnaby W. Greenland , Mark C. Bagley , John Spencer Chemmedchem 59 DOI: 10.1002/cmdc.202100641 Diamond Proposal Number(s): [19301] Open Access Show Abstract ▼ Abstract: The pentafluorosulfanyl (-SF5) functional group is of increasing interest as a bioisostere in medicinal chemistry. A library of SF5-containing compounds, including amide, isoxazole, and oxindole derivatives, was synthesised using a range of solution-based and solventless methods, including microwave and ball-mill techniques. The library was tested against targets including human dihydroorotate dehydrogenase (HDHODH). A subsequent focused approach led to synthesis of analogues of the clinically used disease modifying anti-rheumatic drugs (DMARDs), Teriflunomide and Leflunomide, considered for potential COVID-19 use, where SF5 bioisostere deployment led to improved inhibition of HDHODH compared with the parent drugs. The results demonstrate the utility of the SF5 group in medicinal chemistry.	Feb 2022

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