ArticleAntibiotics (Basel, Switzerland)2023
Semisynthetic Amides of Amphotericin B and Nystatin A
Article in Antibiotics (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 25 citations in OpenAlex.
- Research and Application of the Polyene Macrolide Antibiotic Nystatin.Molecules (Basel, Switzerland) · 2026Review
- Natamycin in Food and Ophthalmology: Knowledge Gaps and Emerging Insights from Zebrafish Models.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Isolation, structure revision and stereochemistry of trichomycins A and B, aromatic analogues of amphotericin B.Scientific reports · 2025Article
- Synergistic antifungal activity of lepidium sativum ZnO nanoparticles and nystatin against resistant candida species.Scientific reports · 2025Article
- Synthesis and Antibacterial Activity of New 6″-Modified Tobramycin Derivatives.Antibiotics (Basel, Switzerland) · 2024Article
- Mono-Antibiotics (Basel, Switzerland) · 2024Article
- Biopolymers as Sustainable and Active Packaging Materials: Fundamentals and Mechanisms of Antifungal Activities.Biomolecules · 2024Review
- Polyene-Based Derivatives with Antifungal Activities.Pharmaceutics · 2024Review
- A Study on the Effect of Quaternization of Polyene Antibiotics' Structures on Their Activity, Toxicity, and Impact on Membrane Models.Antibiotics (Basel, Switzerland) · 2024Article
- Design of Protease-Responsive Antifungal Liposomal Formulation Decorated with a Lipid-Modified Chitin-Binding Domain.International journal of molecular sciences · 2024Article
- Lipid-Centric Approaches in Combating Infectious Diseases: Antibacterials, Antifungals and Antivirals with Lipid-Associated Mechanisms of Action.Antibiotics (Basel, Switzerland) · 2023Review
- Various Biomimetics, Including Peptides as Antifungals.Biomimetics (Basel, Switzerland) · 2023Review
- Article
- Water Quality, Heavy Metals, and Antifungal Susceptibility to Fluconazole of Yeasts from Water Systems.International journal of environmental research and public health · 2023Article
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
Polyene antifungal amphotericin B (AmB) has been used for over 60 years, and remains a valuable clinical treatment for systemic mycoses, due to its broad antifungal activity and low rate of emerging resistance. There is no consensus on how exactly it kills fungal cells but it is certain that AmB and the closely-related nystatin (Nys) can form pores in membranes and have a higher affinity towards ergosterol than cholesterol. Notably, the high nephro- and hemolytic toxicity of polyenes and their low solubility in water have led to efforts to improve their properties. We present the synthesis of new amphotericin and nystatin amides and a comparative study of the effects of identical modifications of AmB and Nys on the relationship between their structure and properties. Generally, increases in the activity/toxicity ratio were in good agreement with increasing ratios of selective permeabilization of ergosterol- vs. cholesterol-containing membranes. We also show that the introduced modifications had an effect on the sensitivity of mutant yeast strains with alterations in ergosterol biosynthesis to the studied polyenes, suggesting a varying affinity towards intermediate ergosterol precursors. Three new water-soluble nystatin derivatives showed a prominent improvement in safety and were selected as promising candidates for drug development.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.