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Anthracene Bisureas as Powerful and Accessible Anion Carriers.
Chemistry - A European Journal ( IF 4.3 ) Pub Date : 2018-04-06 , DOI: 10.1002/chem.201800508
Christopher M Dias 1 , Hennie Valkenier 2 , Anthony P Davis 1
Affiliation  

Synthetic anion carriers (anionophores) have potential as biomedical research tools and as treatments for conditions arising from defective natural transport systems (notably cystic fibrosis). Highly active anionophores that are readily accessible and easily deliverable are especially valuable. Previous work has resulted in steroid and trans-decalin based anionophores with exceptional activity for chloride/nitrate exchange in vesicles, but poor accessibility and deliverability. This work shows that anthracene 1,8-bisureas can fulfil all three criteria. In particular, a bis-nitrophenyl derivative is prepared in two steps from commercial starting materials, yet shows comparable transport activity to the best currently known. Moreover, unlike earlier highly active systems, it does not need to be preincorporated in test vesicles but can be introduced subsequent to vesicle formation. This transporter also shows the ability to transfer between vesicles, and is therefore uniquely effective for anion transport at low transporter loadings. The results suggest that anthracene bisureas are promising candidates for application in biological research and medicine.

中文翻译:

蒽双脲作为强大且易于使用的阴离子载体。

合成阴离子载体(阴离子载体)具有作为生物医学研究工具和治疗因自然运输系统缺陷(特别是囊性纤维化)引起的疾病的潜力。容易获得且易于递送的高活性阴离子载体尤其有价值。先前的工作已经产生了基于类固醇和反式十氢化萘的阴离子载体,其在囊泡中具有优异的氯/硝酸盐交换活性,但可及性和递送性较差。这项工作表明蒽 1,8-双脲可以满足所有三个标准。特别是,双硝基苯基衍生物是由商业起始材料分两步制备的,但显示出与目前已知的最佳转运活性相当的转运活性。此外,与早期的高活性系统不同,它不需要预先掺入测试囊泡中,而是可以在囊泡形成后引入。该转运蛋白还显示出在囊泡之间转移的能力,因此对于低转运蛋白负载下的阴离子转运特别有效。结果表明,蒽双脲是生物研究和医学应用的有希望的候选者。
更新日期:2018-04-06
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