{"title":"经典手性开关战略之死只是夸大其词","authors":"Israel Agranat, Ilaria D'Acquarica","doi":"10.1021/acsmedchemlett.4c00450","DOIUrl":null,"url":null,"abstract":"<p><p>The strategy of classical chiral switches of drugs is still alive, contrary to a 2024 <i>Journal of Medicinal Chemistry</i> Perspective on approved chiral drugs claiming its death. Surveys of approved chiral-switch and racemic drugs should be based on reports of global regulatory authorities, not just FDA and EMA, which revealed overlooked chiral switches and racemates. The approved antihypertensive racemate nebivolol indicates the synergy between its enantiomers, highlighting the advocacy of developing racemic drugs.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 11","pages":"1797-1801"},"PeriodicalIF":4.0000,"publicationDate":"2024-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11571025/pdf/","citationCount":"0","resultStr":"{\"title\":\"The Death of the Strategy of Classical Chiral Switches Is an Exaggeration.\",\"authors\":\"Israel Agranat, Ilaria D'Acquarica\",\"doi\":\"10.1021/acsmedchemlett.4c00450\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The strategy of classical chiral switches of drugs is still alive, contrary to a 2024 <i>Journal of Medicinal Chemistry</i> Perspective on approved chiral drugs claiming its death. Surveys of approved chiral-switch and racemic drugs should be based on reports of global regulatory authorities, not just FDA and EMA, which revealed overlooked chiral switches and racemates. The approved antihypertensive racemate nebivolol indicates the synergy between its enantiomers, highlighting the advocacy of developing racemic drugs.</p>\",\"PeriodicalId\":20,\"journal\":{\"name\":\"ACS Medicinal Chemistry Letters\",\"volume\":\"15 11\",\"pages\":\"1797-1801\"},\"PeriodicalIF\":4.0000,\"publicationDate\":\"2024-10-10\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11571025/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Medicinal Chemistry Letters\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acsmedchemlett.4c00450\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/11/14 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acsmedchemlett.4c00450","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/11/14 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
The Death of the Strategy of Classical Chiral Switches Is an Exaggeration.
The strategy of classical chiral switches of drugs is still alive, contrary to a 2024 Journal of Medicinal Chemistry Perspective on approved chiral drugs claiming its death. Surveys of approved chiral-switch and racemic drugs should be based on reports of global regulatory authorities, not just FDA and EMA, which revealed overlooked chiral switches and racemates. The approved antihypertensive racemate nebivolol indicates the synergy between its enantiomers, highlighting the advocacy of developing racemic drugs.
期刊介绍:
ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to:
Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics)
Biological characterization of new molecular entities in the context of drug discovery
Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc.
Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry
Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources
Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response
Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic
Mechanistic drug metabolism and regulation of metabolic enzyme gene expression
Chemistry patents relevant to the medicinal chemistry field.