小心 N-苯甲酰氧基苯甲酰胺。

IF 4.2 2区化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Molecules Pub Date : 2024-10-31 DOI:10.3390/molecules29215143

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

{"title":"小心 N-苯甲酰氧基苯甲酰胺。","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","doi":"10.3390/molecules29215143","DOIUrl":null,"url":null,"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.","PeriodicalId":19041,"journal":{"name":"Molecules","volume":"29 21","pages":""},"PeriodicalIF":4.2000,"publicationDate":"2024-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11548001/pdf/","citationCount":"0","resultStr":"{\"title\":\"Beware of N-Benzoyloxybenzamides.\",\"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\",\"doi\":\"10.3390/molecules29215143\",\"DOIUrl\":null,\"url\":null,\"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.\",\"PeriodicalId\":19041,\"journal\":{\"name\":\"Molecules\",\"volume\":\"29 21\",\"pages\":\"\"},\"PeriodicalIF\":4.2000,\"publicationDate\":\"2024-10-31\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11548001/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecules\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.3390/molecules29215143\",\"RegionNum\":2,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecules","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.3390/molecules29215143","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}

引用次数: 0

摘要

经过高通量筛选以发现酸性神经酰胺酶抑制剂，我们报告了新型和极强的共价抑制剂 1。在重新合成和稳定性监测之后，我们发现 1 的化学性质不稳定，在室温下会与 DMSO 发生反应。这种分解方式可能是这一类化合物的普遍现象，因此我们建议在药物发现研究中谨慎使用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文本刊更多论文

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, 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.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Molecules 化学-有机化学

CiteScore

7.40

自引率

8.70%

发文量

7524

审稿时长

1.4 months

期刊介绍： Molecules (ISSN 1420-3049, CODEN: MOLEFW) is an open access journal of synthetic organic chemistry and natural product chemistry. All articles are peer-reviewed and published continously upon acceptance. Molecules is published by MDPI, Basel, Switzerland. Our aim is to encourage chemists to publish as much as possible their experimental detail, particularly synthetic procedures and characterization information. There is no restriction on the length of the experimental section. In addition, availability of compound samples is published and considered as important information. Authors are encouraged to register or deposit their chemical samples through the non-profit international organization Molecular Diversity Preservation International (MDPI). Molecules has been launched in 1996 to preserve and exploit molecular diversity of both, chemical information and chemical substances.