Malaria, in particular infection with P. falciparum (the most lethal of the human malaria parasite species, responsible for nearly one million deaths every year), is one of the most devastating and common infectious disease throughout the world. Beginning with quinine, quinoline containing compounds have long been used in clinical treatment of malaria and remained the mainstays of chemotherapy against malaria. The emergence of P. falciparum strains resistant to almost all antimalarials prompted medicinal chemists and biologists to study their effective replacement with an alternative mechanism of action and new molecules. Combination with variety of quinolines and other active moieties may increase the antiplasmodial and antimalarial activities and reduce the side effects. Thus, hybridization is a very attractive strategy to develop novel antimalarials. This review aims to summarize the recent advances towards the discovery of antiplasmodial and antimalarial hybrids including quinoline skeleton to provide an insight for rational designs of more active and less toxic quinoline hybrids antimalarials.

疟疾，特别是恶性疟原虫（人类疟疾中最致命的寄生虫物种，每年造成近一百万例死亡）感染，是全世界最毁灭性和最常见的传染病之一。从奎宁开始，含有喹啉的化合物长期以来一直用于疟疾的临床治疗，并且仍然是抗疟疾化学疗法的主要手段。恶性疟原虫的出现对几乎所有抗疟药都有抗药性的菌株促使药用化学家和生物学家研究用另一种作用机理和新分子有效替代它们的方法。与各种喹啉和其他活性部分结合使用可增加抗疟原虫和抗疟疾的活性，并减少副作用。因此，杂交是发展新型抗疟疾的非常有吸引力的策略。这篇综述旨在总结发现包括喹啉骨架在内的抗疟原虫和抗疟疾杂种的最新进展，从而为合理设计更具活性和毒性较小的喹啉杂种抗疟药提供见识。