Jefford Charles W
Department of Organic Chemistry, University of Geneva, 1211 Geneva, Switzerland.
Drug Discov Today. 2007 Jun;12(11-12):487-95. doi: 10.1016/j.drudis.2007.04.009. Epub 2007 May 7.
The present review describes the current status of synthetic cyclic peroxides, trioxanes and trioxolanes that show significant promise as antimalarial drugs because of their artemisinin-like activity. The literature from 1996 onwards is critically surveyed to provide an update on how an age-old, persistent, debilitating and frequently deadly disease could be treated by new, affordable and effective medicines possessing the peroxide pharmacophore. The review is not exhaustive and does not cover recent progress on the lead structure artemisinin and its derivatives. Nevertheless, some mechanistic aspects gleaned from artemisinin that have relevance to synthetic peroxides are discussed.
本综述描述了合成环状过氧化物、三恶烷和三恶茂烷的现状,这些化合物因其类似青蒿素的活性而有望成为抗疟药物。对1996年以来的文献进行了批判性综述,以更新关于如何用具有过氧化物药效团的新型、经济有效药物治疗这种古老、持久、使人衰弱且常常致命的疾病的信息。本综述并不详尽,也未涵盖先导结构青蒿素及其衍生物的最新进展。尽管如此,还讨论了从青蒿素中收集到的一些与合成过氧化物相关的作用机制方面的内容。