靛红类化合物的抗疟疾活性

Isatin Derivatives and Their Antiplasmodial as Well as Antimalarial Activities

疟疾是全球性传染病,每年约有5亿人罹患疟疾,死亡近百万。尽管临床上使用的抗疟药物对药敏型疟疾疗效显著,但是耐药疟原虫的出现使得这类药物的疗效逐年下降。因此,有必要研发新型抗疟药。靛红具有多种生物活性,广泛存在于药物分子中。近年来的研究表明,靛红类化合物具有潜在的抗疟疾活性,引起了药物化学家的极大兴趣。本文将归纳近年来靛红类化合物在抗疟疾领域的研究进展,并讨论这类化合物的构-效关系,为更合理的设计抗疟新药提供理论帮助。

Malaria continues its devastating impact on the health of human populations globally, with around 500 million cases and the death of around 1 million individuals annually. The antimalarials currently used in clinical still highly effective against drug-sensitive infections, while the growing spread of resistance requires new and effective antimalarials. Isatins, which displayed diverse biological activities, also showed potential in vitro antiplasmodial and in vivo antimalarial activities, making them promising candidates for treatment of malaria. This review presents the current progresses of isatin-based derivatives as potential antimalarials as well as their structure- activity relationship to provide insights to develop new antimalarials.