Abstract
Deferasirox, ExJade, is an FDA-approved iron chelator used for the treatment of iron overload. In this work, we report several fluorescent deferasirox derivatives that display unique photophysical properties, i.e., aggregation-induced emission (AIE), excited state intramolecular proton transfer, charge transfer, and through-bond and through-space conjugation characteristics in aqueous media. Functionalization of the phenol units on the deferasirox scaffold afforded the fluorescent responsive pro-chelator ExPhos, which enabled the detection of the disease-based biomarker alkaline phosphatase (ALP). The diagnostic potential of these deferasirox derivatives was supported by bacterial biofilm studies.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaline Phosphatase / analysis
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins / analysis
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Biofilms / drug effects
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Biomarkers / analysis
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Cefoperazone / pharmacology
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Deferasirox / analogs & derivatives*
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Deferasirox / pharmacology
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Deferasirox / radiation effects
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Fluorescent Dyes / chemistry*
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Fluorescent Dyes / pharmacology
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Fluorescent Dyes / radiation effects
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Light
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Methicillin-Resistant Staphylococcus aureus / drug effects
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Methicillin-Resistant Staphylococcus aureus / enzymology
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Methicillin-Resistant Staphylococcus aureus / physiology
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Microbial Sensitivity Tests
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Microscopy, Confocal
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Microscopy, Fluorescence
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Pseudomonas aeruginosa / drug effects
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Pseudomonas aeruginosa / enzymology
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Pseudomonas aeruginosa / physiology
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Sulbactam / pharmacology
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Biomarkers
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Fluorescent Dyes
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Cefoperazone
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Alkaline Phosphatase
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Sulbactam
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Deferasirox