New Broad-spectrum Antibacterial Amphiphilic Aminoglycosides Active Against Resistant Bacteria: From Neamine Derivatives to Smaller Neosamine Analogues
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
View Archive Info| Field | Value | |
| Title |
New Broad-spectrum Antibacterial Amphiphilic
Aminoglycosides Active Against Resistant Bacteria: From
Neamine Derivatives to Smaller Neosamine Analogues
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| Creator |
Zimmermann, Louis
Das, Indrajit Désiré, Jérôme Sautrey, Guillaume Barros R. S., Vinicius Khoury, Micheline El Mingeot-Leclercq, Marie-Paule Décout, Jean-Luc |
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| Subject |
Chemistry
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| Description |
Aminoglycosides (AGs) constitute a major family of potent and broad-spectrum antibiotics disturbing protein synthesis through binding to the A site of 16S rRNA. Decades of widespread clinical use of AGs strongly reduced their clinical efficacy through the selection
of resistant bacteria. Recently, conjugation of lipophilic groups to AGs generated a novel
class of potent antibacterial amphiphilic aminoglycosides (AAGs) with significant improved
activities against various sensitive and resistant bacterial strains. We have identified
amphiphilic 3’,6-dialkyl derivatives of the small aminoglycoside neamine as broad spectrum
antibacterial agents targeting bacterial membranes. Here, we report on the synthesis and the
activity against sensitive and resistant Gram-negative and/or Gram-positive bacteria of new
amphiphilic 3’,4’-dialkyl neamine derivatives and of their smaller analogues in the 6-
aminoglucosamine (neosamine) series prepared from N-acetylglucosamine.
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| Publisher |
American Chemical Society
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| Date |
2016
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://www.eprints.iicb.res.in/2558/1/acs%252Ejmedchem%252E6b00818.pdf
Zimmermann, Louis and Das, Indrajit and Désiré, Jérôme and Sautrey, Guillaume and Barros R. S., Vinicius and Khoury, Micheline El and Mingeot-Leclercq, Marie-Paule and Décout, Jean-Luc (2016) New Broad-spectrum Antibacterial Amphiphilic Aminoglycosides Active Against Resistant Bacteria: From Neamine Derivatives to Smaller Neosamine Analogues. Journal of Medicinal Chemistry. (In Press) |
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| Relation |
http://dx.doi.org/10.1021/acs.jmedchem.6b00818
http://www.eprints.iicb.res.in/2558/ |
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