The Challenge of Atropisomerism in Drug Discovery

摘要

The modern pharmaceutical industry is profoundly affected by chirality: it is well established that enantiomers may differ significantly in biological activity, pharmacokinetics, and toxicity. The cases of thalidomide and perhexiline, whose enantiomers differ dangerously in effect or metabolic properties, emphasize the importance of addressing stereochemistry in drug development.