ArticleChemMedChem2022
Structure-Activity Relationships for 5'' Modifications of 4,5-Aminoglycoside Antibiotics.
Article in ChemMedChem, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Pangenome analysis ofAntimicrobial agents and chemotherapy · 2026Article
- Article
- Phenotypic Differentiation Within theAntibiotics (Basel, Switzerland) · 2024Article
- Experimental Determination of the pACS omega · 2024Article
- Ototoxicity: a high risk to auditory function that needs to be monitored in drug development.Frontiers in molecular neuroscience · 2024Review
- Thiazolation of phenylthiosemicarbazone to access new thiazoles: anticancer activity and molecular docking.Future medicinal chemistry · 2024Article
- 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
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Authors and funding
9 authors.
Funding
Abstract
Modification at the 5''-position of 4,5-disubstituted aminoglycoside antibiotics (AGAs) to circumvent inactivation by aminoglycoside modifying enzymes (AMEs) is well known. Such modifications, however, unpredictably impact activity and affect target selectivity thereby hindering drug development. A survey of 5''-modifications of the 4,5-AGAs and the related 5-O-furanosyl apramycin derivatives is presented. In the neomycin and the apralog series, all modifications were well-tolerated, but other 4,5-AGAs require a hydrogen bonding group at the 5''-position for maintenance of antibacterial activity. The 5''-amino modification resulted in parent-like activity, but reduced selectivity against the human cytosolic decoding A site rendering this modification unfavorable in paromomycin, propylamycin, and ribostamycin. Installation of a 5''-formamido group and, to a lesser degree, a 5''-ureido group resulted in parent-like activity without loss of selectivity. These lessons will aid the design of next-generation AGAs capable of circumventing AME action while maintaining high antibacterial activity and target selectivity.
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