Synthesis and antibacterial activity of desosamine-modified macrolide derivatives
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- 作者：Nicolas LeTourneau ; Pavan Vimal ; Dorota Klepacki ; Alex ; er Mankin ; Artem Melman
- 关键词：Macrolide antibiotics ; Desosamine ; Erm resistance ; Deoxygenation
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：15 July, 2012
- 年：2012
- 卷：22
- 期：14
- 页码：4575-4578
- 全文大小：522 K
文摘
Structural factors behind erm macrolide resistance were studied through synthesis of new macrolide derivates possessing truncated desosamine sugar moieties and subsequent determination of their antibacterial activity. Synthesized compounds with 2¡ä-deoxy and 3¡ä-desmethyl desosamine rings demonstrated decreased antibacterial activity on the native Staphylococcus aureus strain and were inactive against constitutively resistance S. aureus. The obtained results indicate that steric repulsion between the dimethylated A2058 and desosamine ring cannot be considered as a primary reason for erm-resistance.