ArticleChemMedChem2021
An Advanced Apralog with Increased in vitro and in vivo Activity toward Gram-negative Pathogens and Reduced ex vivo Cochleotoxicity.
Article in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 25 citations in OpenAlex.
- Article
- Synthesis of Methyl Aprabiosaminide and 2-Hydroxyapramycin from Apramycin.Organic letters · 2025Article
- Pulmonary Delivery of Antibiotics to the Lungs: Current State and Future Prospects.Pharmaceutics · 2025Review
- Practical Synthesis from Streptomycin and Regioselective Partial Deprotections of (-)-(1The Journal of organic chemistry · 2024Article
- Benzimidazole as a Privileged Scaffold in Drug Design and Discovery.Current topics in medicinal chemistry · 2024Review
- Synthesis of Gentamicins C1, C2, and C2a and Antiribosomal and Antibacterial Activity of Gentamicins B1, C1, C1a, C2, C2a, C2b, and X2.ACS infectious diseases · 2023Article
- Ribosome-targeting antibiotics and resistanceRSC medicinal chemistry · 2023Review
- Importance of Co-operative Hydrogen Bonding in the Apramycin-Ribosomal Decoding A-Site Interaction.ChemMedChem · 2023Article
- Synthesis, Antibacterial and Antiribosomal Activity of the 3Antibiotics (Basel, Switzerland) · 2022Article
- Structure-Activity Relationships for 5'' Modifications of 4,5-Aminoglycoside Antibiotics.ChemMedChem · 2022Article
- Brief considerations on targeting RNA with small molecules.Faculty reviews · 2022Review
- Structural mechanism of GTPase-powered ribosome-tRNA movement.Nature communications · 2021Article
- Influence of ring size in conformationally restricted ring I analogs of paromomycin on antiribosomal and antibacterial activity.RSC medicinal chemistry · 2021Article
- Synthesis and Antibacterial Activity of Propylamycin Derivatives Functionalized at the 5''- and Other Positions with a View to Overcoming Resistance Due to Aminoglycoside Modifying Enzymes.ACS infectious diseases · 2021Article
- En Route to the Transformation of Glycoscience: A Chemist's Perspective on Internal and External Crossroads in Glycochemistry.Journal of the American Chemical Society · 2021Article
Corrections and comments
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Authors and funding
14 authors at 7 institutions in 3 countries.
Funding
Abstract
We describe the convergent synthesis of a 5-O-β-D-ribofuranosyl-based apramycin derivative (apralog) that displays significantly improved antibacterial activity over the parent apramycin against wild-type ESKAPE pathogens. In addition, the new apralog retains excellent antibacterial activity in the presence of the only aminoglycoside modifying enzyme (AAC(3)-IV) acting on the parent, without incurring susceptibility to the APH(3') mechanism that disables other 5-O-β-D-ribofuranosyl 2-deoxystreptamine type aminoglycosides by phosphorylation at the ribose 5-position. Consistent with this antibacterial activity, the new apralog has excellent 30 nM activity (IC
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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.