Author/Authors :
Sofia Barluenga، نويسنده , , Klaus B. Simonsen، نويسنده , , Ethel S. Littlefield، نويسنده , , Benjamin K. Ayida، نويسنده , , Dionisios Vourloumis، نويسنده , , Geoffrey C. Winters، نويسنده , , Masayuki Takahashi، نويسنده , , Sarah Shandrick، نويسنده , , Qiang Zhao، نويسنده , , Qing Han، نويسنده , , Thomas Hermann، نويسنده ,
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.
Keywords :
antibiotics , Structure-based design.* Corresponding author. Tel.:+1-858-530-3659 , RNA , fax:+1-858-527-1539
