在医疗和兽医应用中过度使用抗菌药物已导致某些微生物产生抗菌药物耐药性，这已成为现代社会的主要问题之一。在这种情况下，使用具有光激活特性的过渡金属配合物作为光触发的药物输送系统，可能成为克服耐药性问题的有效策略。在这项工作中，合成了几种带有三联吡啶配体的钌配合物和克霉唑片段（一种有效的抗真菌药物）。主要目标是探索该配合物作为抗真菌剂的潜在光活化活性，并评估在三联吡啶配体上引入不同取代基的效果。该复合物能够在可见光照射下在短时间内释放克霉唑单元。通过TD-DFT计算解释了取代基对光解速率的影响。这些复合物针对三种不同的酵母进行了测试，这些酵母是根据真菌感染的患病率而选择的。羧基苯单元连接到三联吡啶配体上的复合物在光下对这三种物质表现出最佳活性，最小抑制浓度值为 0.88 μM，光毒性指数为 50。该复合物的活性明显高于游离克霉唑的活性，特别是在可见光照射下（高出 141 倍）。这些复合物对酵母物种的活性比对癌细胞系的活性更高。版权所有 © 2024。由 Elsevier Inc. 出版。

The overuse of antimicrobial agents in medical and veterinary applications has led to the development of antimicrobial resistance in some microorganisms and this is now one of the major concerns in modern society. In this context, the use of transition metal complexes with photoactivatable properties, which can act as drug delivery systems triggered by light, could become a potent strategy to overcome the problem of resistance. In this work several Ru complexes with terpyridine ligands and the clotrimazole fragment, which is a potent antimycotic drug, were synthesized. The main goal was to explore the potential photoactivated activity of the complexes as antifungal agents and evaluate the effect of introducing different substituents on the terpyridine ligand. The complexes were capable of delivering the clotrimazole unit upon irradiation with visible light in a short period of time. The influence of the substituents on the photodissociation rate was explained by means of TD-DFT calculations. The complexes were tested against three different yeasts, which were selected based on their prevalence in fungal infections. The complex in which a carboxybenzene unit was attached to the terpyridine ligand showed the best activity against the three species under light, with minimal inhibitory concentration values of 0.88 μM and a phototoxicity index of 50 achieved. The activity of this complex was markedly higher than that of free clotrimazole, especially upon irradiation with visible light (141 times higher). The complexes were more active on yeast species than on cancer cell lines.Copyright © 2024. Published by Elsevier Inc.