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11,12-氨基甲酸酯-3-O-酰基红霉素衍生物的合成及其抗菌活性

Synthesis and antibacterial activity of 11,12-carbamate-3-O-acyl erythromycin derivatives.

作者信息

Xu Peng, Liu Lu, He Wei, Li Yun, Liu Jian, Lei Ping-Sheng

机构信息

Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, China.

出版信息

J Asian Nat Prod Res. 2009 Oct;11(10):880-97. doi: 10.1080/10286020903176461.

Abstract

A novel series of acylide derivatives have been synthesized which exhibit in vitro potency against key respiratory pathogens. Modification of position 3 was accomplished by replacing different 3-O-substituted acyl groups in the macrolide core via a facile procedure. Compounds 7a-7i were eventually yielded by the conjunction of diverse hetero-aryl side chains with the 11-N,12-O-carbamate sub-structure.

摘要

已经合成了一系列新型的酰化物衍生物,它们对关键呼吸道病原体具有体外活性。通过一种简便的方法,通过取代大环内酯核心中不同的3-O-取代酰基来完成3位的修饰。化合物7a-7i最终通过将不同的杂芳基侧链与11-N,12-O-氨基甲酸酯亚结构结合而得到。

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