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一种新型酮内酯类:先导化合物的合成及抗菌活性

A novel ketolide class: Synthesis and antibacterial activity of a lead compound.

作者信息

Andreotti Daniele, Bientinesi Ilaria, Biondi Stefano, Donati Daniele, Erbetti Isabelle, Lociuro Sergio, Marchioro Carla, Pozzan Alfonso, Ratti Emiliangelo, Terreni Silvia

机构信息

GlaxoSmithKline, Medicine Research Centre, Via A Fleming 4, I-37135 Verona, Italy.

出版信息

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5265-9. doi: 10.1016/j.bmcl.2007.02.019. Epub 2007 Feb 9.

Abstract

Synthesis and antibacterial activity of a new class of ketolide antibiotics, exemplified by the prototype GW680788X (1), are described. The structure of (1) has been elucidated by spectroscopic analysis. The good antibacterial activity shown by (1) in comparison with clarithromycin prompted us to consider this compound as a lead molecule for further exploration.

摘要

描述了一类新型酮内酯抗生素的合成及其抗菌活性,以原型GW680788X(1)为例。通过光谱分析阐明了(1)的结构。与克拉霉素相比,(1)显示出良好的抗菌活性,这促使我们将该化合物视为进一步探索的先导分子。

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