| Literature DB >> 14741274 |
Sofia Barluenga1, Klaus B Simonsen, Ethel S Littlefield, Benjamin K Ayida, Dionisios Vourloumis, Geoffrey C Winters, Masayuki Takahashi, Sarah Shandrick, Qiang Zhao, Qing Han, Thomas Hermann.
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.Entities:
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Year: 2004 PMID： 14741274 DOI： 10.1016/j.bmcl.2003.11.028
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823