Current fragment sets tend to be dominated by flatter molecules, and their shape diversity does not reflect that of the fragments that are theoretically possible. The design and synthesis of a set of bridged fragments containing a bridgehead nitrogen is described. Many of these fragments contain twisted lactams whose modulated electronic properties may present unusual opportunities for interaction with target proteins. The demonstrated novelty, three-dimensionality and molecular properties of the set of 22 fragments may provide valuable, and highly distinctive, starting points for fragment-based drug discovery.

中文翻译：

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基于扭曲双环内酰胺的片段集的设计与合成

当前的片段集倾向于由较平坦的分子控制，并且它们的形状多样性并不反映理论上可能的片段的多样性。描述了一组包含桥头氮的桥连片段的设计和合成。这些片段中许多都含有扭曲的内酰胺，其内在的电子特性调节可能会提供与靶蛋白相互作用的不寻常机会。这组22个片段的新颖性，三维性和分子特性可为基于片段的药物发现提供有价值且高度独特的起点。