Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, PR China.
Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, PR China.
Eur J Med Chem. 2020 May 1;193:112215. doi: 10.1016/j.ejmech.2020.112215. Epub 2020 Mar 9.
Malaria remains a serious worldwide health danger and massive economic trouble to disease-endemic nations. Presently, 250 million of malarial cases are expected worldwide. The emergence of fighting of the Plasmodium parasite against the first-line antimalarial drugs has fueled research attention in the way of designing new scaffolds as well as strategies to counter the drug resistance. Chalcones are simple and well-known analogs, which were found in a huge number of natural compounds and also been prepared according to their suitable synthetic approaches. This review illustrates the current progresses on structure-activity relationship (SAR) and mechanism of diverse types of chalcone derivatives that play a significant role for the development of novel safe, less toxic and highly active antimalarials. This present mini-review will be useful to scientists in research fields of medicinal chemistry, organic synthesis, and also various biological applications particularly for the development of novel antiplasmodial and antimalarial agents.
疟疾仍然是一个严重的全球健康威胁，也是疾病流行国家的巨大经济负担。目前，预计全球将有 2.5 亿例疟疾病例。疟原虫寄生虫对抗一线抗疟药物的斗争的出现引起了人们对设计新支架以及对抗药物耐药性的策略的研究关注。查耳酮是简单而著名的类似物，在大量天然化合物中被发现，并且也根据其合适的合成方法进行了制备。这篇综述说明了不同类型查尔酮衍生物的结构-活性关系（SAR）和作用机制的最新进展，这些衍生物在开发新型安全、低毒和高效的抗疟药物方面发挥了重要作用。这篇简短综述将对药物化学、有机合成以及各种生物学应用领域的科学家有用，特别是对开发新型抗疟原虫和抗疟药物的研究。
