Pinheiro Luiz C S, Feitosa Lívia M, Silveira Flávia F DA, Boechat Nubia
Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos Farmanguinhos, Fundação Oswaldo Cruz, Rio de Janeiro, RJ, Brazil.
An Acad Bras Cienc. 2018;90(1 Suppl 2):1251-1271. doi: 10.1590/0001-3765201820170830.
According to the World Health Organization, malaria remains one of the biggest public health problems in the world. The development of resistance is a current concern, mainly because the number of safe drugs for this disease is limited. Artemisinin-based combination therapy is recommended by the World Health Organization to prevent or delay the onset of resistance. Thus, the need to obtain new drugs makes artemisinin the most widely used scaffold to obtain synthetic compounds. This review describes the drugs based on artemisinin and its derivatives, including hybrid derivatives and dimers, trimers and tetramers that contain an endoperoxide bridge. This class of compounds is of extreme importance for the discovery of new drugs to treat malaria.
根据世界卫生组织的数据，疟疾仍然是世界上最大的公共卫生问题之一。耐药性的发展是当前令人担忧的问题，主要原因是针对该疾病的安全药物数量有限。世界卫生组织推荐以青蒿素为基础的联合疗法来预防或延缓耐药性的出现。因此，获取新药的需求使得青蒿素成为获取合成化合物最广泛使用的骨架。本综述描述了基于青蒿素及其衍生物的药物，包括含有内过氧化物桥的杂化衍生物、二聚体、三聚体和四聚体。这类化合物对于发现治疗疟疾的新药极为重要。
