468065-22-7Relevant articles and documents
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux
Gorityala, Bala Kishan,Guchhait, Goutam,Goswami, Sudeep,Fernando, Dinesh M.,Kumar, Ayush,Zhanel, George G.,Schweizer, Frank
, p. 8441 - 8455 (2016)
Therapeutic interventions to treat multidrug-resistant (MDR) Pseudomonas aeruginosa infections are severely limited and often require the use of colistin as drug of last resort. The major challenges impeding the development of novel antipseudomonal agents
Effects of 5-O-Ribosylation of Aminoglycosides on Antimicrobial Activity and Selective Perturbation of Bacterial Translation
Herzog, Ido M.,Louzoun Zada, Sivan,Fridman, Micha
supporting information, p. 8008 - 8018 (2016/11/15)
We studied six pairs of aminoglycosides and their corresponding ribosylated derivatives synthesized by attaching a β-O-linked ribofuranose to the 5-OH of the deoxystreptamine ring of the parent pseudo-oligosaccharide antibiotic. Ribosylation of the 4,6-disubstituted 2-deoxystreptamine aminoglycoside kanamycin B led to improved selectivity for inhibition of prokaryotic relative to cytosolic eukaryotic in vitro translation. For the pseudodisaccharide aminoglycoside scaffolds neamine and nebramine, ribosylated derivatives were both more potent antimicrobials and more selective to inhibition of prokaryotic translation. On the basis of the results of this study, we suggest that modification of the 5-OH position of the streptamine ring of other natural or semisynthetic pseudodisaccharide aminoglycoside scaffolds containing an equatorial amine at the 2′ sugar position with a β-O-linked ribofuranose is a promising avenue for the development of novel aminoglycoside antibiotics with improved efficacy and reduced toxicity.
Aminoglycoside antibiotics as novel anti-infective agents
-
Page 40, (2010/02/06)
This invention relates to novel aminoglycoside compounds having antibacterial and anti-infective activity and to pharmaceutical compositions, methods of making and methods of treatment employing the same.