- Synthesis and Biological Activity of Mono- and Di-N-acylated Aminoglycosides
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Despite issues with oto/nephrotoxicity and bacterial resistance, aminoglycosides (AGs) remain an effective and widely used class of antibacterial agents. For decades now, efforts toward the development of novel AGs with potential to overcome some of these
- Chandrika, Nishad Thamban,Green, Keith D.,Houghton, Jacob L.,Garneau-Tsodikova, Sylvie
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supporting information
p. 1134 - 1139
(2015/11/24)
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- Structure-based design, synthesis and A-site rRNA co-crystal complexes of novel amphiphilic aminoglycoside antibiotics with new binding modes: A synergistic hydrophobic effect against resistant bacteria
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Incorporation of an hydrophobic (phenethylamino)ethyl ether at C2″ of N1-(HABA)-3′,4′-dideoxyparomomycin led to a novel analog with an excellent antibacterial profile against a host of resistant bacteria.
- Hanessian, Stephen,Pachamuthu, Kandasamy,Szychowski, Janek,Gigure, Alexandre,Swayze, Eric E.,Migawa, Michael T.,Fran?ois, Boris,Kondo, Jiro,Westhof, Eric
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supporting information; experimental part
p. 7097 - 7101
(2011/01/03)
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- Design of novel antibiotics that bind to the ribosomal acyltransfer site
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The structure of neamine bound to the A site of the bacterial ribosomal RNA was used in the design of novel aminoglycosides. The design took into account stereo and electronic contributions to interactions between RNA and aminoglycosides, as well as a ran
- Haddad, Jalal,Kotra, Lakshmi P.,Llano-Sotelo, Beatriz,Kim, Choonkeun,Azucena Jr., Eduardo F.,Liu, Meizheng,Vakulenko, Sergei B.,Chow, Christine S.,Mobashery, Shahriar
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p. 3229 - 3237
(2007/10/03)
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- 4-O-(2,3,5-Trideoxy-5-amino-α-D-pentofuranosyl)-6-O-aminoglycosyl-1,3-diaminocyclitois, methods for their preparation, pharmaceutical formulations thereof and their use as antibacterial agents
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4-O-(2,3,5-Trideoxy-5-amino-α-D-pentofuranosyl)-6-O-aminoglycosyl-1,3-diaminocyclitols and 1-N-substituted derivatives thereof are described together with methods for their preparation and their use as antibacterial agents. Preferred are 1-N-(ω-amino-α-hydroxyalkanoyl)-[4-O-(2,3,5-trideoxy-5-amino-α-D-pentofuranosyl)-6-O-garosaminyl-2-deoxystreptamines], particularly the 1-N-(S-β-amino-α-hydroxypropionyl) derivatives, which are broad spectrum antibacterial agents.
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