{"title":"Covalent Conjugation Strategies for Antifungal Agents: Synthetic Approaches and Therapeutic Potential.","authors":"Andrzej S Skwarecki, Marta Skwarecka","doi":"10.1002/cmdc.202500403","DOIUrl":null,"url":null,"abstract":"<p><p>The increasing prevalence of invasive fungal infections, alongside rising resistance to conventional antifungal therapies, necessitates the development of improved treatment strategies. This review provides a comprehensive overview of recent advances in the design, synthesis, and biological evaluation of antifungal drug conjugates. Particular emphasis is placed on structural modifications of clinically used antifungal agents-such as azoles, echinocandins, and polyene macrolides-as well as novel conjugates incorporating coumarins, steroids, amino acids, and peptides. Conjugation strategies, including covalent attachment to small molecules, polymers, or bioactive moieties, have been employed to improve pharmacokinetic properties, reduce toxicity, and overcome drug resistance. The synthesis methods and biological profiles of selected conjugates are critically discussed, highlighting their potential as candidates for next-generation antifungal therapeutics. This review underscores the versatility of conjugation chemistry as a promising platform for antifungal drug development.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202500403"},"PeriodicalIF":3.4000,"publicationDate":"2025-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemMedChem","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1002/cmdc.202500403","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The increasing prevalence of invasive fungal infections, alongside rising resistance to conventional antifungal therapies, necessitates the development of improved treatment strategies. This review provides a comprehensive overview of recent advances in the design, synthesis, and biological evaluation of antifungal drug conjugates. Particular emphasis is placed on structural modifications of clinically used antifungal agents-such as azoles, echinocandins, and polyene macrolides-as well as novel conjugates incorporating coumarins, steroids, amino acids, and peptides. Conjugation strategies, including covalent attachment to small molecules, polymers, or bioactive moieties, have been employed to improve pharmacokinetic properties, reduce toxicity, and overcome drug resistance. The synthesis methods and biological profiles of selected conjugates are critically discussed, highlighting their potential as candidates for next-generation antifungal therapeutics. This review underscores the versatility of conjugation chemistry as a promising platform for antifungal drug development.
期刊介绍:
Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies.
ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs.
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