Tuszewska Helena, Szczepański Jacek, Mandziuk Sławomir, Trotsko Nazar
Chair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4a, Chodzki Str., 20-093 Lublin, Poland.
Department of Clinical Oncology and Chemotherapy, Medical University of Lublin, 8, Jaczewski Str., 20-090 Lublin, Poland.
Bioorg Chem. 2023 Apr;133:106398. doi: 10.1016/j.bioorg.2023.106398. Epub 2023 Jan 30.
Thiazolidin-4-one derivatives have a wide range of therapeutic implementations and clinical significance for medicinal chemistry. This heterocyclic ring has been reported to possess a variety of biological activities, including antiprotozoal activities that have inspired scientists to integrate this scaffold with different pharmacophoric fragments to design novel and effective antiprotozoal compounds. There are reviews describing thiazolidin-4-ones small molecules as good candidates with a single type of antiprotozoal activity, but none of these show collected news associated with the antiprotozoal activity of thiazolidin-4-ones and their SAR analysis from the last decade. In this review we are focusing on the antitoxoplasmic, anti-trypanosomal, antimalarial, antileishmanial, and antiamoebic activity of these derivatives, we attempt to summarize and analyze the recent developments with regard to the antiprotozoal potential of 4-TZD covering the structure-activity relationship and main molecular targets. The importance of various structural modifications at C2, N3, and C5 of the thiazolidine-4-one core has also been discussed in this review. We hope that all information concluded in this review can be useful for other researchers in constructing new effective antiprotozoal agents.
噻唑烷-4-酮衍生物在药物化学领域具有广泛的治疗应用和临床意义。据报道，这个杂环具有多种生物活性，包括抗原虫活性，这激发了科学家们将该骨架与不同的药效基团片段整合，以设计新型有效的抗原虫化合物。有综述将噻唑烷-4-酮小分子描述为具有单一类型抗原虫活性的良好候选物，但这些综述均未展示过去十年中与噻唑烷-4-酮抗原虫活性及其构效关系分析相关的汇总信息。在本综述中，我们聚焦于这些衍生物的抗弓形虫、抗锥虫、抗疟、抗利什曼原虫和抗阿米巴活性，试图总结和分析4-TZD抗原虫潜力的最新进展，涵盖构效关系和主要分子靶点。本综述还讨论了噻唑烷-4-酮核心结构在C2、N3和C5处进行各种结构修饰的重要性。我们希望本综述中总结的所有信息能对其他研究人员构建新型有效的抗原虫药物有所帮助。
