扩大药物再利用/手性转换的范围,二次制药的要素:奎宁/奎尼丁案例

Ilaria D’Acquarica, Israel Agranat
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引用次数: 0

摘要

将药物重新用于新的医疗用途和手性转换是二次制药的要素。本文以抗疟药奎宁和抗心律失常药奎尼丁的非对映准对映历史(1638-2022 年)为基础,拓宽应用范围,重点介绍这两种药物的再利用/手性转换。奎宁,一种基本药物,改变了世界。药物再利用是一种为已批准或在研药物在原医疗适应症范围之外确定新用途的策略。药物再利用的定义中不包括潜在药物。药物再利用可在治疗组内或治疗组外进行,如奎尼丁到奎宁的再利用,从治疗心律失常或严重疟疾到无并发症疟疾的再利用。手性转换的范围包括从外消旋物到单一对映体,以及其他手性状态的转换,如从外消旋物和准外消旋物到鳞片状混合物。奎宁/奎尼丁立体异构体共有 16 种。鉴于金鸡纳生物碱立体异构体具有多种药理活性,本文呼吁对它们进行全面的药物再利用/手性转换搜索,以获得新的医学用途。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Widened scope of drug repurposing/chiral switches, elements of secondary pharmaceuticals: the quinine/quinidine case
Drug repurposing to new medical uses and chiral switches are elements of secondary pharmaceuticals. This article focuses on drug repurposing/chiral switches of the diastereomeric quasi-enantiomeric antimalarial quinine and antiarrhythmic quinidine, based on the histories of these drugs (1638–2022), applying a widened scope. Quinine, an essential medicine, changed the world. Drug repurposing is a strategy for identifying new uses for approved or investigational drugs outside the scope of the original medical indications. Potential drugs are not included in the definition of drug repurposing. Drug repurposing may be within or outside the therapeutic group, e.g., quinidine to quinine repurposing, from treatment of arrhythmia or severe malaria to uncomplicated malaria. The scope of chiral switches included racemate to single enantiomer and other switches of the status of chirality, e.g., racemate and quasi-racemate to scalemic mixtures. There are 16 quinine/quinidine stereoisomers. Given the multiple pharmacological activities of Cinchona alkaloid stereoisomers, this article calls for subjecting them to comprehensive drug repurposing/chiral switch searches for new medical uses.
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