ArticleBioorganic & medicinal chemistry letters2018
Improved potency and reduced toxicity of the antifungal peptoid AEC5 through submonomer modification.
Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Structural Optimization of Antifungal Peptoids targetingACS medicinal chemistry letters · 2025Article
- Article
- Development of an Anti-Biofilm Screening Technique Leads to the Discovery of a Peptoid with Efficacy againstACS infectious diseases · 2022Article
- Discovery and Characterization of a Rapidly Fungicidal and Minimally Toxic Peptoid againstACS medicinal chemistry letters · 2021Article
- Peptoids with Antibiofilm Activity against the Gram Negative Obligate Anaerobe,Molecules (Basel, Switzerland) · 2021Article
- Exploration of the site-specific nature and generalizability of a trimethylammonium salt modification on vancomycin: A-ring derivatives.Tetrahedron · 2019Article
- Toward a clinical antifungal peptoid: Investigations into the therapeutic potential of AEC5.Biopolymers · 2019Article
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Authors and funding
3 authors.
Funding
Abstract
As proteolytically stable peptidomimetics, peptoids could serve as antifungal agents to supplement a therapeutic field wrought with toxicity issues. We report the improvement of an antifungal peptoid, AEC5, through an iterative structure-activity relationship study. A sarcosine scan was used to first identify the most pharmacophorically important peptoid building blocks of AEC5, followed by sequential optimization of each building block. The optimized antifungal peptoid from this study, β-5, has improved potency towards Cryptococcus neoformans and decreased toxicity towards mammalian cells. For example, the selectivity ratio for C. neoformans over mammalian fibroblasts was improved from 8 for AEC5 to 37 for β-5.
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