Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics
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- 作者：Henninger ; Todd C. ; Xu ; Xiaodong ; Abbanat ; Darren ; Baum ; Ellen Z. ; Foleno ; Barbara D. ; Hilliard ; Jamese J. ; et. al.
- 关键词：Ketolide ; Carbamate ; Antibiotics ; Resistant bacteria
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2004
- 出版时间：September 6, 2004
- 年：2004
- 卷：14
- 期：17
- 页码：4495-4499
- 全文大小：294 K
文摘
A new series of antibacterial ketolides is reported, which features the use of a C-6 carbamate for tethering the arylalkyl sidechain to the macrolide core. The best members of this series display in vitro and in vivo activity comparable to telithromycin. Partial epimerization at C-2, unobserved in previously reported ketolides, was noted for this series.