Synthesis and Biological Evaluation of a Teixobactin Analogue
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- 作者：Yahya E. Jad ; Gerardo A. Acosta ; Tricia Naicker ; Melissa Ramtahal ; Ayman El-Faham ; Thavendran Govender ; Hendrik G. Kruger ; Beatriz G. de la Torre ; Fernando Albericio
- 刊名：Organic Letters
- 出版年：2015
- 出版时间：December 18, 2015
- 年：2015
- 卷：17
- 期：24
- 页码：6182-6185
- 全文大小：314K
- ISSN：1523-7052
文摘
The first synthesis and biological activity of a teixobactin analogue is reported. Substitution of the unusual lass="smallcaps">l-allo-enduracididine residue by the naturally occurring lass="smallcaps">l-arginine was achieved, and the analogue gave an activity trend similar to that of teixobactin (against Gram-postive bacteria) and meropenem, which was approved by the FDA in 1996. The synthetic route used allows for the synthesis of the natural product as well as the development of a program of medicinal chemistry.