Synthesis and Biological Evaluation of a Teixobactin Analogue
Synthesis and Biological Evaluation of a Teixobactin Analogue
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DOI：
10.1021/acs.orglett.5b03176
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发表时间：
2015-12-18
期刊：
影响因子：
5.2
通讯作者：
Albericio, Fernando
中科院分区：
文献类型：
--
作者：
Jad, Yahya E.;Acosta, Gerardo A.;Albericio, Fernando
报道了一种teixobactin类似物的首次合成及其生物活性。用天然存在的l-精氨酸取代了不寻常的l- alloo -enduracididine残基，其类似物的活性趋势与1996年FDA批准的teixobactin（抗革兰氏阳性细菌）和美罗培南相似。所使用的合成路线允许天然产物的合成以及药物化学程序的发展。
The first synthesis and biological activity of a teixobactin analogue is reported. Substitution of the unusual l-allo-enduracididine residue by the naturally occurring 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.