Shandong Institute of Parasitic Diseases, Shandong First Medical University & Shandong Academy of Medical Sciences, Jining, Shandong, China.
Department of Vector Biological Control, Jining Municipal Center for Disease Control and Prevention, Jining, Shandong, China.
Arch Pharm (Weinheim). 2020 Apr;353(4):e1900350. doi: 10.1002/ardp.201900350. Epub 2020 Jan 31.
Malaria, one of the most striking, re-emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug-resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure-activity relationship of these compounds are also discussed.
疟疾是由疟原虫属引起的最显著、重新出现的传染病之一，给全球医疗保健系统带来了巨大负担。控制和消除疟疾的主要挑战是不断出现越来越广泛的耐药性疟疾，因此迫切需要开发新的抗疟药物。查尔酮衍生物在自然界中无处不在，由于其多样化的生物特性，已成为药物化学应用中不可或缺的单元。许多查尔酮衍生物表现出体外和体内抗疟活性的潜力，因此查尔酮可以作为开发新型抗疟药物的有用模板。本综述涵盖了作为抗疟药物的查尔酮杂合体的最新发展。还讨论了这些化合物的设计和构效关系的关键方面。
