794524-05-3Relevant articles and documents
High-throughput assay for quantification of aminoglycoside-Ribosome interaction
Yamashita, Shun,Bergmann, Dominik,Sato, Ayato,Nomoto, Mika,Tada, Yasuomi,Humpf, Hans-Ulrich,Itami, Kenichiro,Hagihara, Shinya
, p. 1048 - 1050 (2016)
The serious side effects of aminoglycosides and the spread of aminoglycoside-resistant strains have restricted the clinical application of aminoglycosides. A compound with the identical mode of action with aminoglycosides and with different molecular skeleton would be an alternative drug for aminoglycosides. In this study, we constructed an SPR-based high-throughput screening system for the discovery of such compounds.
MEMBRANE-TARGETING AMINOGLYCOSIDE-BASED CATIONIC AMPHIPHILES AND THERAPEUTIC USES
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Page/Page column 52; 58, (2014/02/15)
The present invention relates to amphiphilic aminoglycoside (AG) derivatives, especially derivatives of tobramycin, kanamycin A and paromomycin comprising hydrophobic side chains linked to the AG moiety by various linkers. These novel derivatives are useful as broad spectrum antibacterial agents targeting bacterial cell membranes, while having minimal toxicity due to non-selective targeting of eukaryotic cell membranes. The present invention further relates to methods for preparing the novel derivatives, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as membrane-targeting antibacterial agents for treating bacterial infections, and for inhibiting bio film growth.
Di-alkylated paromomycin derivatives: Targeting the membranes of Gram positive pathogens that cause skin infections
Berkov-Zrihen, Yifat,Herzog, Ido M.,Feldman, Mark,Sonn-Segev, Adar,Roichman, Yael,Fridman, Micha
, p. 3624 - 3631 (2013/07/11)
A collection of paromomycin-based di-alkylated cationic amphiphiles differing in the lengths of their aliphatic chain residues were designed, synthesized, and evaluated against 14 Gram positive pathogens that are known to cause skin infections. Paromomyci
Conformational constraint as a means for understanding RNA-aminoglycoside specificity
Blount, Kenneth F.,Zhao, Fang,Hermann, Thomas,Tor, Yitzhak
, p. 9818 - 9829 (2007/10/03)
The lack of high RNA target selectivity displayed by aminoglycoside antibiotics results from both their electrostatically driven binding mode and their conformational adaptability. The inherent flexibility around their glycosidic bonds allows them to easi