入侵性真菌感染(IFIs)正日益威胁公共卫生，并与高发病率和死亡率相关。 IFIs在接受化疗的癌症患者中也是常见并发症。然而，有效且安全的抗真菌药物仍然有限，严重的耐药性进一步削弱了抗真菌治疗的疗效。因此，迫切需要新的抗真菌药物来治疗危及生命的真菌疾病，特别是具有新作用模式、有利的药代动力学特征和抗耐药性活性的真菌病。在本综述文章中，我们总结了新的抗真菌靶点和靶向抑制剂设计，重点关注它们的抗真菌活性、选择性和机理。我们还阐述了用于改善抗真菌药物的物理化学和药代动力学特征的前体药设计策略。双重靶向抗真菌药物提供了一种治疗耐药感染和癌症相关真菌感染的新策略。版权所有©2023 Elsevier B.V.

Invasive fungal infections (IFIs) are emerging as a serious threat to public health and are associated with high incidence and mortality. IFIs also represent a frequent complication in patients with cancer who are undergoing chemotherapy. However, effective and safe antifungal agents remain limited, and the development of severe drug resistance further undermines the efficacy of antifungal therapy. Therefore, there is an urgent need for novel antifungal agents to treat life-threatening fungal diseases, especially those with new mode of action, favorable pharmacokinetic profiles, and anti-resistance activity. In this review, we summarize new antifungal targets and target-based inhibitor design, with a focus on their antifungal activity, selectivity, and mechanism. We also illustrate the prodrug design strategy used to improve the physicochemical and pharmacokinetic profiles of antifungal agents. Dual-targeting antifungal agents offer a new strategy for the treatment of resistant infections and cancer-associated fungal infections.Copyright © 2023 Elsevier B.V. All rights reserved.