An Overview on Antifilarial Efficacy of Heterocyclic Motifs Encompassing Synthetic Strategies, SAR, and Commercialized Medications.

IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Current topics in medicinal chemistry Pub Date : 2024-11-01 DOI:10.2174/0115680266321838241024073444
Sumit Tahlan, Sucheta Singh, Kailash C Pandey
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Abstract

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 Wuchereria bancrofti, Brugia malayi, and Brugia timori, 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.

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杂环基团的抗丝虫药效概述,包括合成策略、SAR 和商业化药物。
丝虫病是最古老、最危险、最致残、最毁容的疾病之一,也是经常被忽视的热带疾病。它有一系列临床症状,死亡率低,发病率高,造成社会歧视。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。淋巴丝虫病由班氏乌切瑞绦虫(Wuchereria bancrofti)、马来氏布鲁格绦虫(Brugia malayi)和蒂莫里氏布鲁格绦虫(Brugia timori)引起,是一种致残性疾病,具有严重的社会和经济后果。尽管使用了传统的抗丝虫药物(如乙酰甲胺嗪(DEC)、阿苯达唑和伊维菌素,这些药物主要是微丝蚴杀虫剂),但感染依然存在。目前的治疗方法(伊维菌素、乙酰甲胺嗪和阿苯达唑)对成虫的疗效有限,而且会产生副作用,因此迫切需要创新的抗丝虫药物。因此,需要大丝虫杀虫剂、胚胎抑制剂和改良的微丝杀虫剂。以下文章讨论了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、药物化学家和制药科学家开发新的、有效的抗丝虫疗法。这篇综述有助于确定新的先导化合物,并优化现有的商业药物以提高其疗效。本综述中涉及的大部分研究涉及丝虫病的形式、寄生虫的生命周期、症状、用于治疗丝虫病的药物、合成方案、SAR 以及报告的研究成果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
期刊介绍: Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
期刊最新文献
Computer-aided Drug Discovery of Epigenetic Modulators in Dual-target Therapy of Multifactorial Diseases. An Overview on Antifilarial Efficacy of Heterocyclic Motifs Encompassing Synthetic Strategies, SAR, and Commercialized Medications. An Insight into the Structure-Activity Relationship of Benzimidazole and Pyrazole Derivatives as Anticancer Agents. Hydroxamic Acids Derivatives: Greener Synthesis, Antiureolytic Properties And Potential Medicinal Chemistry Applications - A Concise Review. Targeting c-Met in Cancer Therapy: Unravelling Structure-Activity Relationships and Docking Insights for Enhanced Anticancer Drug Design.
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