Beware of <i>N</i>-Benzoyloxybenzamides

Beware of <i>N</i>-Benzoyloxybenzamides

Following a High-Throughput Screening campaign to discover inhibitors of acid ceramidase, we report the novel and extremely potent covalent inhibitor, <b>1</b>. Following resynthesis and stability monitoring, we discovered that <b>1</b> is chemically unstable and reacts with...

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Bibliographic Details
Main Authors: 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
Format: Article
Language:English
Published: MDPI AG 2024-10-01
Series:Molecules
Subjects:
<i>N</i>-benzoyloxybenzamides
acid ceramidase
PAINS
Online Access:https://www.mdpi.com/1420-3049/29/21/5143
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Summary:Following a High-Throughput Screening campaign to discover inhibitors of acid ceramidase, we report the novel and extremely potent covalent inhibitor, <b>1</b>. Following resynthesis and stability monitoring, we discovered that <b>1</b> 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.
ISSN:1420-3049

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