Design and synthesis of a fragment set based on twisted bicyclic lactams

Publication date: Available online 22 February 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Haitham Hassan, Stephen P. Marsden, Adam Nelson
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.

Graphical abstract

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