Synthesis of New Tyrosol‐Based Phosphodiester Derivatives: Effect on Amyloid β Aggregation and Metal Chelation Ability
作者:Valeria Romanucci、Maddalena Giordano、Gaetano De Tommaso、Mauro Iuliano、Roberta Bernini、Mariangela Clemente、Sara Garcia‐Viñuales、Danilo Milardi、Armando Zarrelli、Giovanni Di Fabio
DOI:10.1002/cmdc.202000807
日期:2021.4.8
suitable tyrosol building blocks and exploiting the well‐established phosphoramidite chemistry. The antioxidant activity of new TPDs has been tested as well as their ability to inhibit Aβ protein aggregation. In addition, their metal chelating ability has been evaluated as a possible strategy to develop new natural‐based entities for the prevention or therapy of AD. Interestingly, TPDs containing a catechol
阿尔茨海默病 (AD) 是一种多因素病理,需要能够解决其特殊性质的多方面药物。越来越多的证据表明,淀粉样蛋白 β (Aβ) 的聚集和氧化应激密切相关,它们的调节可能在对比 AD 相关损伤方面具有积极和协同作用。在此,从合适的酪醇结构单元开始,利用成熟的亚磷酰胺化学,开发了一种新的、基于片段的、基于片段的酪醇磷酸二酯衍生物(TPDs)方法。已经测试了新 TPD 的抗氧化活性以及它们抑制 Aβ 蛋白聚集的能力。此外,它们的金属螯合能力已被评估为开发新的天然实体以预防或治疗 AD 的可能策略。40和强大的螯合生物金属如 Cu II和 Zn II 的能力。