6-O-杂芳基氨基甲酰基-11,12-内酯酮类化合物的合成及其抗菌活性
Synthesis and antibacterial activity of 6-O-heteroarylcarbamoyl-11,12-lactoketolides.
作者信息
Grant Eugene B, Guiadeen Deodialsingh, Abbanat Darren, Foleno Barbara D, Bush Karen, Macielag Mark J
机构信息
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 1;16(7):1929-33. doi: 10.1016/j.bmcl.2005.12.097. Epub 2006 Jan 30.
A new series of erythromycin A derivatives, the 6-O-heteroarylcarbamoyl-11,12-lactoketolides, with activity against macrolide-resistant streptococci, are described. Structurally, these macrolide antibiotics are characterized by a heteroaryl side chain attached to the macrolactone core through a carbamate linkage at the C6 position, as well as 11,12-gamma-lactone and 3-keto functionalities. The synthesis and antibacterial activity of this new series of ketolides are discussed.
本文描述了一系列新型红霉素A衍生物，即6-O-杂芳基氨基甲酰基-11,12-内酯酮类化合物，它们对耐大环内酯类链球菌具有活性。从结构上看，这些大环内酯类抗生素的特征在于通过C6位的氨基甲酸酯键连接到大环内酯核心的杂芳基侧链，以及11,12-γ-内酯和3-酮官能团。本文还讨论了这一系列新型酮内酯类化合物的合成及其抗菌活性。
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