Enduracididine, a rare amino acid component of peptide antibiotics: Natural products and synthesis.
Enduracididine, a rare amino acid component of peptide antibiotics: Natural products and synthesis.
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DOI：
10.3762/bjoc.12.226
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发表时间：
2016
影响因子：
2.7
通讯作者：
Brimble MA
中科院分区：
文献类型：
--
作者：
Atkinson DJ;Naysmith BJ;Furkert DP;Brimble MA
对当前临床抗菌剂的耐药性不断上升，是对全球公共健康的迫在眉睫的威胁，并突显了对新的先导化合物的需求，以用于药物发现。其中一种潜在的先导化合物是多肽抗生素teixobactin，它最近从一种未培养的细菌来源中分离出来，对广泛的耐药病原体表现出非常高的效力，但没有明显的耐药性。Teixobactin的一种稀有氨基酸残基成分耐尿酸二丁已知只存在于少数也具有良好抗生素活性的天然产品中。本文重点介绍了耐尿酸地丁在天然产物中的存在及其生物合成，并对其类似物进行了综述。讨论了已报道的研究耐尿酸地丁的环胍结构的合成方法，说明了迄今为止在开发有效的合成路线以促进药物发现方面所遇到的挑战，这些努力是受teixobactin的发现启发的。
Rising resistance to current clinical antibacterial agents is an imminent threat to global public health and highlights the demand for new lead compounds for drug discovery. One such potential lead compound, the peptide antibiotic teixobactin, was recently isolated from an uncultured bacterial source, and demonstrates remarkably high potency against a wide range of resistant pathogens without apparent development of resistance. A rare amino acid residue component of teixobactin, enduracididine, is only known to occur in a small number of natural products that also possess promising antibiotic activity. This review highlights the presence of enduracididine in natural products, its biosynthesis together with a review of analogues of enduracididine. Reported synthetic approaches to the cyclic guanidine structure of enduracididine are discussed, illustrating the challenges encountered to date in the development of efficient synthetic routes to facilitate drug discovery efforts inspired by the discovery of teixobactin.