Beware of N-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 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.
Authors
- Mari Davies
- Emyr Lloyd‐Evans (ORCID: https://orcid.org/0000-0002-3626-1611)
- D. Heulyn Jones (ORCID: https://orcid.org/0000-0002-4290-2999)
- Helen Waller‐Evans (ORCID: https://orcid.org/0000-0003-4133-6064)
- Jonathan Cubitt (ORCID: https://orcid.org/0000-0002-7420-4351)
- Simon E. Ward (ORCID: https://orcid.org/0000-0002-8745-8377)
- Sian E. Gardiner (ORCID: https://orcid.org/0000-0001-7815-7321)
- Ross Riseley
- Benson M. Kariuki (ORCID: https://orcid.org/0000-0002-8658-3897)
- Gerry Evans
Institutions
- Cardiff University (GB)
Publication Details
- Journal
- Molecules
- Published
- 2024-10-31
- DOI
- https://doi.org/10.3390/molecules29215143
- Citations
- 1
- Primary Topic
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Type
- article
- Field-Weighted Citation Impact
- 0.25