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引用次数: 0
摘要
一半以上的药物是手性化合物,其手性决定了其分子相互作用、生态环保安全性和有效性。总体而言,近 90% 的手性化合物是以外消旋体的形式上市销售的,外消旋体由两种对映体的等摩尔混合物组成。尽管外消旋体具有相同的化学结构和化学键,但它们在手性环境中的功能却各不相同,在药理学、毒理学、新陈代谢和药代动力学等生物特性方面也表现出明显的差异。近年来,随着不对称合成技术的发展,人们对开发用于药物化学的手性药物分子的单一对映体产生了浓厚的兴趣。在这篇综述中,我们将以 2022 年和 2023 年美国 FDA 批准的手性药物为例,重点介绍这些药物的合成及其手性诱导和对映体过量的信息。
The significance of chirality in contemporary drug discovery-a mini review
More than half of drugs are chiral compounds with their chirality determining their molecular interactions, ecofriendly environmental safety and efficacy. Overall nearly 90% of chiral compounds are marketed as racemates consisting of an equimolar mixture of two enantiomers. Despite having identical chemical structure and bonding, racemates function differently when exposed to chiral environments and demonstrate notable variances in biological properties such as pharmacology, toxicology, metabolism and pharmacokinetics, etc. Advancements in asymmetric synthesis in recent years have led to considerable interest in the development of single enantiomers of chiral drug molecules for medicinal chemistry settings. In this review, we want to compile examples of chiral medicines approved by the FDA in the years 2022 and 2023 with an emphasis on their synthesis along with information on chiral induction as well as enantiomeric excess.
期刊介绍:
An international, peer-reviewed journal covering all of the chemical sciences, including multidisciplinary and emerging areas. RSC Advances is a gold open access journal allowing researchers free access to research articles, and offering an affordable open access publishing option for authors around the world.