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
本研究的目的是对一种新型的基于正电荷的酰胺键构象固定进行广泛的应用和评价。因此,氨基烷基侧链的连接代表了一种更具仿生性的结构修饰,就像以前实现酰胺键构象固定的策略中的情况一样。因此,以这种方式修饰的多肽和蛋白质很可能会被相应的受体(或通常是靶结构)耐受。如第一个例子所示,新的原理产生了相对较强的固定效应,可以在药物化学和合成化学领域中加以利用。
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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