Rational design of azepane-glycoside antibiotics targeting the bacterial ribosome.
نویسندگان
چکیده
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.
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عنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 14 3 شماره
صفحات -
تاریخ انتشار 2004