Synthesis and biological activity of new 5-O-sugar modified ketolide and 2-fluoro-ketolide antibiotics
摘要:
A series of new triazole-containing ketolides and 2-fluoro-ketolides in which the 5-O-desosamine was replaced by unnatural sugars were synthesized and evaluated against relevant macrolide-sensitive and macrolide-resistant respiratory pathogens. Excellent in vitro antibacterial activities were demonstrated for ketolide analogues having the 6'-OBz-3'-dimethylamino-glucose and 6'-OBz-4'-deoxy-3'-dimethylamino-glucose substituents. (c) 2005 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2005.01.027
作为产物:
描述:
11-N-(4-azido-butyl)-6-O-methyl-5-(2,6-dibenzoyl-3N-Fmoc-4-deoxy-glucopyranosyl)-2-fluoro-3-oxo-erythronolide A 11,12-carbamate 在
哌啶 作用下,
以
N,N-二甲基甲酰胺 为溶剂,
生成
参考文献:
名称:
Synthesis and biological activity of new 5-O-sugar modified ketolide and 2-fluoro-ketolide antibiotics
摘要:
A series of new triazole-containing ketolides and 2-fluoro-ketolides in which the 5-O-desosamine was replaced by unnatural sugars were synthesized and evaluated against relevant macrolide-sensitive and macrolide-resistant respiratory pathogens. Excellent in vitro antibacterial activities were demonstrated for ketolide analogues having the 6'-OBz-3'-dimethylamino-glucose and 6'-OBz-4'-deoxy-3'-dimethylamino-glucose substituents. (c) 2005 Elsevier Ltd. All rights reserved.