Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing, China.
Chirality. 2022 Oct;34(10):1355-1370. doi: 10.1002/chir.23497. Epub 2022 Jul 29.
Chirality is one of the key factors affecting the medicinal efficacy of compounds. In addition to central chirality, sterically hindered chiral axes commonly appear in drugs and the resulting chirality is known as atropisomerism. With developments in medicinal chemistry, atropisomerism has attracted increasing attention. This review discusses the classification, biological activity, pharmacokinetics, toxicity and side effects of atropisomers, and can serve as a reference in the research and development of potential chiral drugs.
手性是影响化合物药效的关键因素之一。除了中心手性外，空间位阻手性轴在药物中也很常见，由此产生的手性被称为对映异构现象。随着药物化学的发展，对映异构现象引起了越来越多的关注。本文综述了对映异构体的分类、生物活性、药代动力学、毒性和副作用，可为潜在手性药物的研究和开发提供参考。
