Conformational fixation of amide bonds through positive charges

通过正电荷对酰胺键进行构象固定

• 批准号: 340628755
• 负责人: Professor Dr. Markus Heinrich
• 金额: --
• 依托单位: Department Chemie und Pharmazie
• 依托单位国家: 德国
• 项目类别: Research Grants
• 财政年份: 2017
• 资助国家: 德国
• 起止时间: 2016-12-31 至 2020-12-31
• 项目状态: 已结题
• 来源: https://gepris.dfg.de/gepris/projekt/340628755?language=en
• 关键词: Conformational; fixation; amide; bonds; through

The aim of the research work is the broad application and evaluation of a novel type of conformational fixation of amide bonds, which is based on positive charges. The attachment of an aminoalkyl side chain thereby represents a much more biomimetic structural modification as it has been the case in previous strategies to achieve conformational fixation of amide bonds. It is thus likely that peptides and proteins, which are modified in this way, will be tolerated by the corresponding receptors (or generally target structures). As shown in first examples, the new principle leads to comparably strong fixation effects, which could be exploited in the fields of medicinal chemistry as well as in synthetic chemistry.

研究工作的目的是广泛应用和评价一种新型的基于正电荷的酰胺键构象固定。因此，氨基烷基侧链的连接代表了一种更加仿生的结构修饰，因为它已经在以前的策略中实现了酰胺键的构象固定。因此，以这种方式修饰的肽和蛋白质很可能被相应的受体（或一般的靶结构）耐受。如第一个例子所示，新原理产生了较强的固定效应，可用于药物化学和合成化学领域。