Department of Chemistry & Biochemistry, University of California Santa Cruz, CA 95064, USA.
Future Med Chem. 2009 Jul;1(4):593-617. doi: 10.4155/fmc.09.56.
Malaria remains one of the most serious global infectious diseases, with an estimated 2 billion people at risk and 1 million deaths annually. Drug resistance is hampering the effectiveness of many current antimalarial therapies and resistant strains of the parasite are now known for almost all classes of antimalarial compounds. Owing to a lack of concerted drug-discovery efforts over the last 30 years, the development pipeline is limited and the identification of new antimalarial lead compounds is a pressing concern. The development of new antimalarials that exhibit novel modes of action is of critical importance if the devastating effects of malaria are to be controlled. Natural products have traditionally played an important role in antimalarial drug development and the marine environment represents an underexplored resource in this regard. This review covers developments in the field of antimalarial drug discovery from marine sources between January 2003 and December 2008 and offers a comprehensive overview of all marine-derived compounds from this period. Marine natural products represent an emerging opportunity in the development of new antimalarial lead compounds. This review provides examples of several recent lead discovery projects that show promise in this regard and presents a perspective on areas of possible future study.
疟疾仍然是全球最严重的传染病之一，估计有 20 亿人面临风险，每年有 100 万人死亡。耐药性正在削弱许多当前抗疟疗法的有效性，目前几乎所有类别的抗疟化合物都存在寄生虫耐药株。由于过去 30 年来缺乏协调一致的药物发现工作，药物研发管道受到限制，寻找新的抗疟先导化合物是当务之急。如果要控制疟疾的毁灭性影响，开发具有新作用模式的新型抗疟药物至关重要。天然产物在抗疟药物开发中一直发挥着重要作用，而海洋环境在这方面是一个尚未充分开发的资源。本综述涵盖了 2003 年 1 月至 2008 年 12 月期间从海洋来源中发现的抗疟药物的发展情况，并全面概述了这一时期所有海洋衍生化合物。海洋天然产物代表了开发新型抗疟先导化合物的一个新机遇。本综述提供了几个近期的发现项目的例子，这些项目在这方面显示出了前景，并提出了未来可能的研究领域的观点。
