Molecules
(Oct 2024)
Beware of <i>N</i>-Benzoyloxybenzamides
Jonathan Cubitt,
Mari Davies,
Ross Riseley,
Gabrielle Evans,
Sian E. Gardiner,
Benson M. Kariuki,
Simon E. Ward,
Emyr Lloyd-Evans,
Helen Waller-Evans,
D. Heulyn Jones
Affiliations
Jonathan Cubitt
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Mari Davies
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Ross Riseley
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Gabrielle Evans
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Sian E. Gardiner
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Benson M. Kariuki
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Simon E. Ward
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Emyr Lloyd-Evans
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
Helen Waller-Evans
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
D. Heulyn Jones
Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
DOI
https://doi.org/10.3390/molecules29215143
Journal volume & issue
Vol. 29,
no. 21
p.
5143
Abstract
Read online
Following a High-Throughput Screening campaign to discover inhibitors of acid ceramidase, we report the novel and extremely potent covalent inhibitor, 1. Following resynthesis and stability monitoring, we discovered that 1 is chemically unstable and reacts with DMSO at room temperature. This mode of decomposition is likely general for this class of compound, and we urge caution for their use in drug discovery research.
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