Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Mumbai, 400019, Maharashtra, India.
Future Med Chem. 2023 Nov;15(22):2113-2141. doi: 10.4155/fmc-2023-0188. Epub 2023 Nov 6.
Given that mitochondrial dysregulation is a biomarker of many cancers, cationic quaternary phosphonium salt (QPS) conjugation is a widely utilized strategy for anticancer drug design. QPS-conjugated compounds exhibit greater cell permeation and accumulation in negatively charged mitochondria, and thus, show enhanced activity. Phylogenetic similarities between mitochondria and bacteria have provided a rationale for exploring the antibacterial properties of mitochondria-targeted compounds. Additionally, due to the importance of mitochondria in the survival of pathogenic microbes, including fungi and parasites, this strategy can be extended to these organisms as well. This review examines recent literature on the antimicrobial activities of various QPS-conjugated compounds and provides future directions for exploring the medicinal chemistry of these compounds.
鉴于线粒体功能紊乱是许多癌症的生物标志物,因此带正电荷的季铵盐(QPS)缀合是一种广泛用于抗癌药物设计的策略。QPS 缀合物在带负电荷的线粒体中具有更好的细胞通透性和积累,因此表现出增强的活性。线粒体与细菌之间的系统发育相似性为探索靶向线粒体的化合物的抗菌特性提供了依据。此外,由于线粒体对于包括真菌和寄生虫在内的病原微生物的生存至关重要,因此该策略也可以扩展到这些生物体。本文综述了近期关于各种 QPS 缀合物的抗菌活性的文献,并为探索这些化合物的药物化学提供了未来的方向。