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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Bibliographische Detailangaben
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.
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Beschreibung
Zusammenfassung:	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.
ISSN:	1433-7851 1521-3773
DOI:	10.1002/anie.200351354