Design and Synthesis of Paromomycin-Related Heterocycle-Substituted Aminoglycoside Mimetics Based on a Mass Spectrometry RNA-Binding Assay

A good starting point for the design of potent bactericidal compounds is the aminoglycoside paromomycin (1). The A‐ring (shown in red) was replaced with a range of heterocycles. An ESIMS‐based RNA‐binding assay was used to screen the binding affinities of the products.

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Veröffentlicht in:Angewandte Chemie International Edition 2003-07, Vol.42 (29), p.3409-3412
Hauptverfasser: Ding, Yili, Hofstadler, Steven A., Swayze, Eric E., Risen, Lisa, Griffey, Richard H.
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container_end_page 3412
container_issue 29
container_start_page 3409
container_title Angewandte Chemie International Edition
container_volume 42
creator Ding, Yili
Hofstadler, Steven A.
Swayze, Eric E.
Risen, Lisa
Griffey, Richard H.
description A good starting point for the design of potent bactericidal compounds is the aminoglycoside paromomycin (1). The A‐ring (shown in red) was replaced with a range of heterocycles. An ESIMS‐based RNA‐binding assay was used to screen the binding affinities of the products.
doi_str_mv 10.1002/anie.200351354
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source Wiley-Blackwell Journals; MEDLINE
subjects aminoglycosides
Aminoglycosides - chemical synthesis
Aminoglycosides - chemistry
Aminoglycosides - metabolism
antibiotics
Binding, Competitive
Carbohydrate Sequence
Drug Design
heterocycles
Ligands
mass spectrometry
Models, Chemical
Molecular Sequence Data
Molecular Structure
Paromomycin - chemistry
RNA, Ribosomal, 16S - chemistry
RNA, Ribosomal, 16S - metabolism
RNA, Ribosomal, 18S - chemistry
RNA, Ribosomal, 18S - metabolism
Spectrometry, Mass, Electrospray Ionization - methods
Structure-Activity Relationship
Substrate Specificity
synthesis design
title Design and Synthesis of Paromomycin-Related Heterocycle-Substituted Aminoglycoside Mimetics Based on a Mass Spectrometry RNA-Binding Assay
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