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Updated: Jun 7, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Beware of N-Benzoyloxybenzamides
Jonathan Cubitt1, Mari Davies1, Ross Riseley1
1Medicines Discovery Institute, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK.
Abstract:
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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