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Importance of the 6'-hydroxy group and its configuration for apramycin activity


Mandhapati, Appi Reddy; Shcherbakov, Dimitri; Duscha, Stefan; Vasella, Andrea; Böttger, Erik C; Crich, David (2014). Importance of the 6'-hydroxy group and its configuration for apramycin activity. ChemMedChem, 9(9):2074-2083.

Abstract

A series of apramycin derivatives was prepared and investigated for antibacterial activity and the ability to inhibit protein synthesis in cell-free translation assays. The effect of various modifications at the 6'- and N7'-positions on antiribosomal activity is discussed in terms of their influence on drug binding to specific residues in the decoding A-site. These studies contribute to the development of a structure-activity relationship for the antibacterial activity of the apramycin class of aminoglycosides and to the future design and development of more active and less toxic antibiotics.

Abstract

A series of apramycin derivatives was prepared and investigated for antibacterial activity and the ability to inhibit protein synthesis in cell-free translation assays. The effect of various modifications at the 6'- and N7'-positions on antiribosomal activity is discussed in terms of their influence on drug binding to specific residues in the decoding A-site. These studies contribute to the development of a structure-activity relationship for the antibacterial activity of the apramycin class of aminoglycosides and to the future design and development of more active and less toxic antibiotics.

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6 citations in Scopus®
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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:04 Faculty of Medicine > Institute of Medical Microbiology
Dewey Decimal Classification:570 Life sciences; biology
610 Medicine & health
Date:September 2014
Deposited On:02 Dec 2014 14:45
Last Modified:05 Apr 2016 18:33
Publisher:Wiley-Blackwell Publishing, Inc.
ISSN:1860-7179
Free access at:Publisher DOI. An embargo period may apply.
Publisher DOI:https://doi.org/10.1002/cmdc.201402146
PubMed ID:25045149

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