Searching for Conjugates as New Structures for Antifungal Therapies,Journal of Medicinal Chemistry

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Searching for Conjugates as New Structures for Antifungal Therapies
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-03-12 , DOI: 10.1021/acs.jmedchem.3c01750
Izabela Muszalska-Kolos ₁ , Piotr Mariusz Dwiecki _{1,

2}

Affiliation

The progressive increase in fungal infections and the decrease in the effectiveness of current therapy explain research on new drugs. The synthesis of compounds with proven antifungal activity, favorable physicochemical and pharmacokinetic properties affecting their pharmaceutical availability and bioavailability, and limiting or eliminating side effects has become the goal of many studies. The publication describes the directions of searching for new compounds with antifungal activity, focusing on conjugates. The described modifications include, among others, azoles or amphotericin B in combination with fatty acids, polysaccharides, proteins, and synthetic polymers. The benefits of these combinations in terms of activity, mechanism of action, and bioavailability were indicated. The possibilities of creating or using nanoparticles, “umbrella” conjugates, siderophores (iron-chelating compounds), and monoclonal antibodies were also presented. Taking into account the role of vaccinations in prevention, the scope of research related to developing a vaccine protecting against fungal infections was also indicated.

中文翻译：

寻找缀合物作为抗真菌疗法的新结构

真菌感染的逐渐增加和当前治疗效果的下降解释了对新药的研究。合成具有经过验证的抗真菌活性、影响其药物利用度和生物利用度的有利理化和药代动力学特性以及限制或消除副作用的化合物已成为许多研究的目标。该出版物描述了寻找具有抗真菌活性的新化合物的方向，重点是缀合物。所描述的修饰包括唑类或两性霉素B与脂肪酸、多糖、蛋白质和合成聚合物的组合等。指出了这些组合在活性、作用机制和生物利用度方面的益处。还提出了创建或使用纳米颗粒、“伞”缀合物、铁载体（铁螯合化合物）和单克隆抗体的可能性。考虑到疫苗接种在预防中的作用，还指出了与开发预防真菌感染的疫苗相关的研究范围。

更新日期：2024-03-12

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