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经典手性转换策略的消亡是一种夸张的说法。

The Death of the Strategy of Classical Chiral Switches Is an Exaggeration.

作者信息

Agranat Israel, D'Acquarica Ilaria

机构信息

Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Rome 00185, Italy.

出版信息

ACS Med Chem Lett. 2024 Oct 10;15(11):1797-1801. doi: 10.1021/acsmedchemlett.4c00450. eCollection 2024 Nov 14.

Abstract

The strategy of classical chiral switches of drugs is still alive, contrary to a 2024 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.

摘要

与一篇2024年关于已批准手性药物的观点文章声称其已消亡相反,经典的药物手性转换策略仍然存在。对已批准的手性转换药物和外消旋药物的调查应基于全球监管机构的报告,而不仅仅是美国食品药品监督管理局(FDA)和欧洲药品管理局(EMA)的报告,这些报告揭示了被忽视的手性转换药物和外消旋体。已批准的抗高血压外消旋药物奈必洛尔表明了其对映体之间的协同作用,突出了开发外消旋药物的主张。

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本文引用的文献

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Chirality of New Drug Approvals (2013-2022): Trends and Perspectives.新药批准的手性(2013-2022):趋势与展望。
J Med Chem. 2024 Feb 22;67(4):2305-2320. doi: 10.1021/acs.jmedchem.3c02239. Epub 2024 Feb 12.
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Anti-infectives Developed as Racemic Drugs in the 21st Century: Norm or Exception?21世纪开发的外消旋体抗感染药物:常态还是例外?
ACS Med Chem Lett. 2023 Jun 12;14(7):875-878. doi: 10.1021/acsmedchemlett.3c00214. eCollection 2023 Jul 13.
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Sulfoxides in medicine.医学中的亚砜类化合物。
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The Quest for Secondary Pharmaceuticals: Drug Repurposing/Chiral-Switches Combination Strategy.寻找二线药物:药物再利用/手性转换组合策略。
ACS Pharmacol Transl Sci. 2023 Jan 17;6(2):201-219. doi: 10.1021/acsptsci.2c00151. eCollection 2023 Feb 10.

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