Search Results - "Fridman, Micha"
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Cationic Pillararenes Potently Inhibit Biofilm Formation without Affecting Bacterial Growth and Viability
Published in Journal of the American Chemical Society (27-01-2016)“…It is estimated that up to 80% of bacterial infections are accompanied by biofilm formation. Since bacteria in biofilms are less susceptible to antibiotics…”
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2
Guiding Drugs to Target‐Harboring Organelles: Stretching Drug‐Delivery to a Higher Level of Resolution
Published in Angewandte Chemie International Edition (28-10-2019)“…The ratio between the dose of drug required for optimal efficacy and the dose that causes toxicity is referred to as the therapeutic window. This ratio can be…”
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3
Benzylic Dehydroxylation of Echinocandin Antifungal Drugs Restores Efficacy against Resistance Conferred by Mutated Glucan Synthase
Published in Journal of the American Chemical Society (06-04-2022)“…Each year, infections caused by fungal pathogens claim the lives of about 1.6 million people and affect the health of over a billion people worldwide. Among…”
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4
Di-N-Methylation of Anti-Gram-Positive Aminoglycoside-Derived Membrane Disruptors Improves Antimicrobial Potency and Broadens Spectrum to Gram-Negative Bacteria
Published in Angewandte Chemie International Edition (09-11-2015)“…The effect of di‐N‐methylation of bacterial membrane disruptors derived from aminoglycosides (AGs) on antimicrobial activity is reported. Di‐N‐methylation of…”
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5
Tuning the Effects of Bacterial Membrane Permeability through Photo‐Isomerization of Antimicrobial Cationic Amphiphiles
Published in Chemistry : a European journal (18-09-2017)“…Several important antimicrobial drugs act by permeabilizing cell membranes. In this study, we showed that the intensity of membrane permeability caused by…”
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6
Fluorescent Tracking of the Endoplasmic Reticulum in Live Pathogenic Fungal Cells
Published in ACS chemical biology (21-12-2018)“…In fungal cells, the endoplasmic reticulum (ER) harbors several of the enzymes involved in the biosynthesis of ergosterol, an essential membrane component,…”
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Chiral Fluorescent Antifungal Azole Probes Detect Resistance, Uptake Dynamics, and Subcellular Distribution in Candida Species
Published in JACS Au (26-08-2024)“…Azoles are essential for fungal infection treatment, yet the increasing resistance highlights the need for innovative diagnostic tools and strategies to…”
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8
Real-Time Imaging of the Azole Class of Antifungal Drugs in Live Candida Cells
Published in ACS chemical biology (21-07-2017)“…Azoles are the most commonly used class of antifungal drugs, yet where they localize within fungal cells and how they are imported remain poorly understood…”
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9
Site-Selective Displacement of Tobramycin Hydroxyls for Preparation of Antimicrobial Cationic Amphiphiles
Published in Organic letters (20-12-2013)“…A short site-selective strategy for the activation and derivatization of alcohols of the clinically important aminoglycoside tobramycin is reported. The choice…”
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10
Spirostrain-Accelerated Chemiexcitation of Dioxetanes Yields Unprecedented Detection Sensitivity in Chemiluminescence Bioassays
Published in ACS central science (24-01-2024)“…Chemiluminescence is a fascinating phenomenon that involves the generation of light through chemical reactions. The light emission from…”
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11
One-Pot Chemoenzymatic Cascade for Labeling of the Epigenetic Marker 5-Hydroxymethylcytosine
Published in Chembiochem : a European journal of chemical biology (07-09-2015)“…The epigenetic DNA modification 5‐hydroxymethylcytosine (5‐hmC) is important for the regulation of gene expression during development and in tumorigenesis…”
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Boosting Chemiexcitation of Phenoxy-1,2-dioxetanes through 7‑Norbornyl and Homocubanyl Spirofusion
Published in JACS Au (23-09-2024)“…The chemiluminescent light-emission pathway of phenoxy-1,2-dioxetane luminophores is increasingly attracting the scientific community’s attention. Dioxetane…”
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Elevated Vacuolar Uptake of Fluorescently Labeled Antifungal Drug Caspofungin Predicts Echinocandin Resistance in Pathogenic Yeast
Published in ACS central science (28-10-2020)“…Echinocandins are the newest class of antifungal drugs in clinical use. These agents inhibit β-glucan synthase, which catalyzes the synthesis of β-glucan, an…”
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14
Exploring the Substrate Promiscuity of Drug-Modifying Enzymes for the Chemoenzymatic Generation of N-Acylated Aminoglycosides
Published in Chembiochem : a European journal of chemical biology (04-01-2010)“…Aminoglycosides are broad-spectrum antibiotics commonly used for the treatment of serious bacterial infections. Decades of clinical use have led to the…”
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15
Antimycobacterial activity of DNA intercalator inhibitors of Mycobacterium tuberculosis primase DnaG
Published in Journal of antibiotics (01-03-2015)“…Owing to the rise in drug resistance in tuberculosis combined with the global spread of its causative pathogen, Mycobacterium tuberculosis ( Mtb ), innovative…”
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Poacic Acid, a Plant-Derived Stilbenoid, Augments Cell Wall Chitin Production, but Its Antifungal Activity Is Hindered by This Polysaccharide and by Fungal Essential Metals
Published in Biochemistry (Easton) (16-04-2024)“…Climate and environmental changes have modified the habitats of fungal pathogens, inflicting devastating effects on livestock and crop production…”
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Deciphering the Biological Activities of Antifungal Agents with Chemical Probes
Published in Angewandte Chemie International Edition (13-03-2023)“…The growing number of fungal infections caused by pathogens resistant to one or more classes of antifungal drugs emphasizes the threat that these…”
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Characterization of Rhodosaminyl Transfer by the AknS/AknT Glycosylation Complex and Its Use in Reconstituting the Biosynthetic Pathway of Aclacinomycin A
Published in Journal of the American Chemical Society (29-08-2007)“…The tetracyclic core of anthracycline natural products with antitumor activity such as aclacinomycin A are tailored during biosynthesis by regioselective…”
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The relationship between the structure and toxicity of aminoglycoside antibiotics
Published in Bioorganic & medicinal chemistry letters (01-07-2020)“…[Display omitted] Aminoglycoside antibiotics, used to treat persistent gram-negative infections, tuberculosis, and life-threatening infections in neonates and…”
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20
One-Pot Synthesis of Glucosamine Oligosaccharides
Published in Organic letters (24-01-2002)“…Tuning the reactivity of glycosyl donors derived from 2-amino-2-deoxy glucose by selective introduction of different N-protecting (NPhth and NHTroc) and…”
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