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Hydroxamate siderophores: Natural occurrence, chemical synthesis, iron binding affinity and use as Trojan horses against pathogens.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-09-05 , DOI: 10.1016/j.ejmech.2020.112791
Danah Al Shaer 1 , Othman Al Musaimi 1 , Beatriz G de la Torre 2 , Fernando Albericio 3
Affiliation  

Hydroxamic acids are an important class of molecules, in particular because of their metal-chelating ability. Microorganisms, including pathogenic bacteria, use hydroxamate-based entities (siderophores), among others, to acquire Fe (III). The “Trojan horse” strategy exploits the need of bacteria for this metal by using Fe (III) active transporters to carry antibacterial or bactericidal moieties into the bacterial cell. Many natural Trojan horses (sideromycins) are derived from hydroxamic acids, thereby reflecting their potency. Various artificial sideromycins and their antibacterial activities have been reported. This review discusses the structural aspects of the hydroxamate-siderophores isolated in the last two decades, the chemical synthesis of their building blocks, their binding affinity towards Fe (III), and their application as Trojan horses (weaknesses and strengths).



中文翻译:

异羟肟酸酯铁载体:天然存在,化学合成,铁结合亲和力,并用作对抗病原体的特洛伊木马。

异羟肟酸是一类重要的分子,特别是由于它们的金属螯合能力。微生物,包括病原细菌,使用基于异羟肟酸酯的实体(铁载体)来获取铁(III)。“特洛伊木马”策略通过使用Fe(III)活性转运蛋白将抗菌或杀菌部分带入细菌细胞,从而开发了对这种金属的细菌需求。许多天然特洛伊木马(Sideromycins)都来自异羟肟酸,从而反映出它们的功效。已经报道了各种人造铁霉素及其抗菌活性。这篇评论讨论了过去二十年中分离的异羟肟酸酯-铁载体的结构方面,其组成部分的化学合成,它们对铁(III)的结合亲和力,

更新日期:2020-09-15
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