手性转换在手性药物研究中的应用

Chiral switch:single enantiomer drugs from racemates

手性药物的单一异构体的研究和开发已经成为药物化学研究的热点领域。许多单一异构体药物的研制过程通过"手性转换"从已有的消旋药物中分离出来。通过上市消旋体药物不同的药理作用和代谢产物3个方面综述了手性转换在手性药物研究中的进展。

Over the last ten to fifteen years, most of the new chiral drugs available on the market currently have been consisting of single enantiomers, rather than the racemic mixtures. As a result of advances in the chemical technologies associated with the synthesis, separation and analysis of the individual enantiomers, the use of single enantiomers has become an area of considerable interest. Many new single-enantiomer drugs are derived from ＂chiral switches＂ of established racemates. A well-timed chiral switch can offer enhanced therapy and further profitability as a ＂ line extension＂ of a major racemic drug with patents that are expiring.