Conformational fixation of amide bonds through positive charges
Conformational fixation of amide bonds through positive charges
批准号:
340628755
负责人:
Professor Dr. Markus Heinrich
金额:
$0.0万
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
项目状态:
已结题
起止时间:
2016-12-31 至 2020-12-31
中文摘要
研究工作的目的是广泛的应用和评估的一种新型的构象固定的酰胺键,这是基于正电荷。因此,氨基烷基侧链的连接代表了更仿生的结构修饰,因为它在先前的策略中是实现酰胺键构象固定的情况。因此,以这种方式修饰的肽和蛋白质可能会被相应的受体(或通常的靶结构)耐受。 如第一个实施例所示,新的原理导致非常强的固定效果,这可以在药物化学和合成化学领域中利用。
英文摘要
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.
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