Institute of Chemistry, University of Silesia, 75. Pułku Piechoty 1, 41-500 Chorzów, Poland.
Department of Biotransformation, Faculty of Biotechnology, University of Wroclaw, Joliot-Curie 14a, 50-383 Wroclaw, Poland.
Molecules. 2020 Jan 15;25(2):345. doi: 10.3390/molecules25020345.
Styrylquinolines are heterocyclic compounds that are known for their antifungal and antimicrobial activity. Metal complexation through hydroxyl groups has been claimed to be a plausible mechanism of action for these types of compounds. A series of novel structures with protected hydroxyl groups have been designed and synthesized to verify the literature data. Their antifungal activity against wild-type strain and mutants with silenced efflux pumps activity has been determined. Combinations with fluconazole revealed synergistic interactions that were dependent on the substitution pattern. These results open a new route for designing active antifungal agents on a styrylquinoline scaffold.
苯乙烯基喹啉是一类具有抗真菌和抗菌活性的杂环化合物。通过羟基进行金属络合被认为是这类化合物的一种合理作用机制。为了验证文献数据，设计并合成了一系列带有保护羟基的新型结构。测定了它们对野生型菌株和沉默外排泵活性的突变体的抗真菌活性。与氟康唑的联合使用显示出协同相互作用，这取决于取代模式。这些结果为设计基于苯乙烯基喹啉骨架的有效抗真菌剂开辟了新途径。
