A nonneglectable stereochemical factor in drug development: Atropisomerism

Chirality. 2022 Oct;34(10):1355-1370. doi: 10.1002/chir.23497. Epub 2022 Jul 29.

Abstract

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.

Keywords: atropisomerism; axial chirality; chiral drug; configuration assignment; stereochemistry.

Publication types

  • Review

MeSH terms

  • Stereoisomerism*