Tahlan Sumit, Singh Sucheta, Pandey Kailash C
ICMR-National Institute of Malaria Research, New Delhi - 110077, India.
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak-124001, India.
Curr Top Med Chem. 2025;25(11):1303-1350. doi: 10.2174/0115680266321838241024073444.
Filariasis is one of the oldest, most dangerous, debilitating, disfiguring diseases and often ignores tropical disorders. It presents with a range of clinical symptoms, a low death rate, and a high morbidity rate, which contributes to social discrimination. This condition has major effects on people's socioeconomic circumstances. This illness is carried by mosquitoes that have spread malaria. Lymphatic filariasis, caused by , and , is a crippling illness with serious social and economic consequences. The infection persisted despite therapy with conventional antifilarial medications such as diethylcarbamazine (DEC), albendazole, and ivermectin, which are mostly microfilaricides. Current treatments (ivermectin, diethylcarbamazine, and albendazole) have limited effectiveness against adult parasites and produce side effects; therefore, innovative antifilarial medications are urgently required. Hence, macrofilaricides, embryostatic agents, and improved microfilaricides are required. The following article discusses the typical synthetic methodologies established for antifilarial activity as well as their marketed pharmaceuticals, which will help researchers, medicinal chemists, and pharmaceutical scientists to develop new and effective antifilarial therapies. This review can help to identify new lead compounds and optimize existing commercial medications to improve their therapeutic efficacy. The majority of the studies addressed in this review concern the forms of filariasis, parasite life cycle, symptoms, medications used to treat filariasis, synthetic schemes, SAR, and results from the reported research.
丝虫病是最古老、最危险、使人衰弱、毁容的疾病之一，常被视为热带疾病。它表现出一系列临床症状，死亡率低但发病率高，这导致了社会歧视。这种疾病对人们的社会经济状况有重大影响。这种疾病由传播疟疾的蚊子携带。由班氏丝虫、马来丝虫和帝汶丝虫引起的淋巴丝虫病是一种致残性疾病，会造成严重的社会和经济后果。尽管使用了传统的抗丝虫药物进行治疗，如乙胺嗪（DEC）、阿苯达唑和伊维菌素（这些药物大多是杀微丝蚴剂），感染仍持续存在。目前的治疗方法（伊维菌素、乙胺嗪和阿苯达唑）对成虫的有效性有限且会产生副作用；因此，迫切需要创新的抗丝虫药物。因此，需要开发杀成虫剂、胚胎抑制剂和改进的杀微丝蚴剂。以下文章讨论了已确立的抗丝虫活性的典型合成方法及其上市药物，这将有助于研究人员、药物化学家以及制药科学家开发新的、有效的抗丝虫疗法。这篇综述有助于识别新的先导化合物，并优化现有的商业药物以提高其治疗效果。本综述中涉及的大多数研究关注丝虫病的类型、寄生虫生命周期、症状、用于治疗丝虫病的药物、合成方案、构效关系以及所报道研究的结果。
