Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Punjab, 160 062, India.
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Punjab, 160 062, India.
Eur J Med Chem. 2022 Nov 15;242:114653. doi: 10.1016/j.ejmech.2022.114653. Epub 2022 Aug 10.
Malaria remains a major vector borne disease claiming millions of lives worldwide due to infections caused by Plasmodium sp. Discovery and development of antimalarial drugs have previously been dominated majorly by single drug therapy. The malaria parasite has developed resistance against first line and second line antimalarial drugs used in the single drug therapy. This has drawn attention to find ways to alleviate the disease burden supplanted by combination therapy with multiple drugs to overcome drug resistance. Emergence of resistant strains even against the combination therapy has now mandated the revision of the current antimalarial pharmacotherapy. Research efforts of the past decade led to the discovery and identification of several new structural classes of antimalarial agents with improved biological attributes over the older ones. The following is a comprehensive review, addressed to the new structural classes of heterocyclic and natural compounds that have been identified during the last decade as antimalarial agents. Some of the classes included herein contain one or more pharmacophores amalgamated into a single bioactive scaffold as antimalarial agents, which act upon the conventional and novel targets.
疟疾仍然是一种主要的由媒介传播的疾病,由于疟原虫引起的感染,导致全球数百万人死亡。抗疟药物的发现和开发以前主要由单一药物疗法主导。疟原虫已经对一线和二线抗疟药物产生了耐药性,这些药物用于单一药物疗法。这引起了人们的关注,即需要找到方法来减轻疾病负担,用多种药物联合治疗来克服耐药性。甚至对联合治疗产生耐药性的菌株的出现,现在已经要求修订当前的抗疟药物疗法。过去十年的研究努力导致发现和鉴定了几种新的结构类别抗疟药物,它们具有比旧药物更好的生物学特性。以下是对过去十年中被确定为抗疟药物的杂环和天然化合物的新结构类别的全面综述。本文中包含的一些类别包含一个或多个药效团,合并为一个单一的生物活性支架作为抗疟药物,这些药物作用于传统和新的靶标。