Department of Parasitology, Faculty of Science, Charles University in Prague, BIOCEV, Vestec, Czech Republic.
Biological Chemistry & Drug Discovery, School of Life Sciences, University of Dundee, Dundee, DD1 5EH, UK.
Trends Parasitol. 2024 Sep;40(9):820-828. doi: 10.1016/j.pt.2024.07.003. Epub 2024 Aug 5.
The development of new drug modalities has been facilitated recently by the introduction of boron as a component of organic compounds, and specifically within a benzoxaborale scaffold. This has enabled exploration of new chemical space and the development of effective compounds targeting a broad range of morbidities, including infections by protozoa, fungi, worms, and bacteria. Most notable is the recent demonstration of a single oral dose cure using acoziborole against African trypanosomiasis. Common and species-/structure-specific interactions between benzoxaboroles and parasite species have emerged and provide vital insights into the mechanisms of cidality, as well as potential challenges in terms of resistance and/or side effects. Here, we discuss the literature specific to benzoxaborole studies in parasitic protists and consider unanswered questions concerning this important new drug class.
新型药物模式的发展最近得益于硼作为有机化合物的组成部分的引入,特别是在苯并噁硼烷支架内。这使得能够探索新的化学空间,并开发针对广泛病态的有效化合物,包括原生动物、真菌、蠕虫和细菌感染。最近,使用 acoziborole 对非洲锥虫病进行单次口服剂量治愈的证明就是一个很好的例子。苯并噁硼烷与寄生虫种类之间的常见和种类/结构特异性相互作用已经出现,并为杀菌机制以及耐药性和/或副作用方面的潜在挑战提供了重要的见解。在这里,我们讨论了关于寄生原生动物中苯并噁硼烷研究的文献,并考虑了这个重要新药类别的一些未解决的问题。