Guangdong Engineering & Technology Research Center for Quality and Efficacy Reevaluation of Post-Market Traditional Chinese Medicine, Guangdong Key Laboratory of Plant Resources, School of Life Sciences, Sun Yat-sen University, Guangzhou, Guangdong, 510275, China.
Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, 510260, China.
Eur J Med Chem. 2022 Jul 5;237:114361. doi: 10.1016/j.ejmech.2022.114361. Epub 2022 Apr 8.
Malaria is a prevalent fatal disease in tropical and subtropical regions around the world. Combinations of Artemisinin, folate antagonists, quinolines, and antibiotics are major choices in clinics. Currently, wide range of parasite's resistance necessitates the search for chemical compounds with new structures and novel antimalarial targets. The literature review was performed covering the relevant literatures published from 1966 to 2021. On the basis of structural classification (spiro-peroxides, spiroindolones, spirocyclohexadienones et al.), different types of molecules were summarized with resources, anti-malarial activities, structure-activity relationship, target introductions, resistance, development progress, and synthetic strategies, for the purpose of providing comprehensive information for developing antimalarial drugs to overcome drug resistance and highlighting the importance of the spiral structure in medicinal chemistry.
疟疾是全球热带和亚热带地区流行的致命疾病。青蒿素、叶酸拮抗剂、喹啉类药物和抗生素的联合用药是临床的主要选择。目前,寄生虫的广泛耐药性要求寻找具有新结构和新抗疟靶点的化合物。文献综述涵盖了 1966 年至 2021 年发表的相关文献。基于结构分类(螺环过氧化物、螺吲哚酮、螺环环己二烯酮等),总结了不同类型的分子,包括资源、抗疟活性、构效关系、靶点介绍、耐药性、开发进展和合成策略,旨在为开发抗疟药物以克服耐药性提供全面的信息,并强调螺旋结构在药物化学中的重要性。