Synthesising polar semi-saturated bicyclic heterocycles can lead to better starting points for fragment-based drug discovery (FBDD) programs. We report the application of diverse chemistry to construct bicyclic systems from a common intermediate, where pyrazole, a privileged heteroaromatic able to bind effectively to biological targets, is fused to diverse saturated counterparts. The generated fragments can be further developed either after confirmation of their binding pose or early in the process, as their synthetic intermediates. Essential quality control (QC) for selection of small molecules to add to a fragment library is discussed.
- Fragment-based drug discovery
- synthetic methods
- polar small molecules
- fused-ring systems
- drug discovery
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To Design and Develop Semi-Saturated and Unsaturated Bicyclic Heterocycles for Fragment-Based Drug Discovery (FBDD) CampaignsAuthor: Luise, N., 2019
Supervisor: Wyatt, P. (Supervisor)
Student thesis: Doctoral Thesis › Doctor of Philosophy