Ngece Kwanele, Ntondini Thabisa L, Khwaza Vuyolwethu, Paca Athandwe M, Aderibigbe Blessing A
Department of Chemistry, University of Fort Hare, Alice 5700, Eastern Cape, South Africa.
Pharmaceutics. 2024 Aug 14;16(8):1065. doi: 10.3390/pharmaceutics16081065.
Polyenes are a class of organic compounds well known for their potent antifungal properties. They are effective due to their ability to target and disrupt fungal cell membranes by binding to ergosterol and forming pores. Despite their effectiveness as antifungal drugs, polyenes have several limitations, such as high toxicity to the host cell and poor solubility in water. This has prompted ongoing research to develop safer and more efficient derivatives to overcome such limitations while enhancing their antifungal activity. In this review article, we present a thorough analysis of polyene derivatives, their structural modifications, and their influence on their therapeutic effects against various fungal strains. Key studies are discussed, illustrating how structural modifications have led to improved antifungal properties. By evaluating the latest advancements in the synthesis of polyene derivatives, we highlight that incorporating amide linkers at the carboxylic moiety of polyene molecules notably improves their antifungal properties, as evidenced by derivatives , , , and . This review can help in the design and development of novel polyene-based compounds with potent antifungal activities.
多烯类是一类以其强大的抗真菌特性而闻名的有机化合物。它们之所以有效，是因为能够通过与麦角固醇结合并形成孔道来靶向和破坏真菌细胞膜。尽管多烯类作为抗真菌药物很有效，但也有一些局限性，比如对宿主细胞毒性高以及在水中溶解度差。这促使人们持续开展研究，以开发更安全、更高效的衍生物，在克服这些局限性的同时增强其抗真菌活性。在这篇综述文章中，我们对多烯类衍生物、它们的结构修饰以及它们对针对各种真菌菌株的治疗效果的影响进行了全面分析。讨论了关键研究，阐明了结构修饰是如何带来改善的抗真菌特性的。通过评估多烯类衍生物合成方面的最新进展，我们强调在多烯分子的羧基部分引入酰胺连接基显著改善了它们的抗真菌特性，衍生物 、 、 和 证明了这一点。这篇综述有助于设计和开发具有强大抗真菌活性的新型多烯基化合物。
