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Bioorg Med Chem Lett ; 14(3): 713-8, 2004 Feb 09.
Article in English | MEDLINE | ID: mdl-14741274

ABSTRACT

RNA recognition by natural aminoglycoside antibiotics depends on the 2-deoxystreptamine (2-DOS) scaffold which participates in specific hydrogen bonds with the ribosomal decoding-site target. Three-dimensional structure information has been used for the design of azepane-monoglycosides, building blocks for novel antibiotics in which 2-DOS is replaced by a heterocyclic scaffold. Azepane-glycosides showed target binding and translation inhibition in the low micromolar range and inhibited growth of Staphylococcus aureus, including aminoglycoside-resistant strains.


Subject(s)
Anti-Bacterial Agents/metabolism , Anti-Bacterial Agents/pharmacology , Azepines/chemistry , Azepines/pharmacology , RNA, Ribosomal/antagonists & inhibitors , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development , Aminoglycosides/adverse effects , Aminoglycosides/chemistry , Anti-Bacterial Agents/chemistry , Azepines/metabolism , Drug Design , Glycosides/chemistry , Glycosides/metabolism , Glycosides/pharmacology , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/metabolism , Heterocyclic Compounds/pharmacology , Nucleic Acid Conformation , Paromomycin , Protein Biosynthesis/drug effects , RNA, Bacterial/antagonists & inhibitors , RNA, Ribosomal/chemistry , Structure-Activity Relationship
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