Generation of Polar Semi-Saturated Bicyclic Pyrazoles for Fragment-Based Drug Discovery Campaigns

Nicola Luise, Paul Wyatt (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)
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Abstract

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.
Original languageEnglish
Pages (from-to)10443-10451
Number of pages9
JournalChemistry: a European Journal
Volume24
Issue number41
Early online date7 May 2018
DOIs
Publication statusPublished - 20 Jul 2018

Keywords

  • Fragment-based drug discovery
  • synthetic methods
  • polar small molecules
  • pyrazole
  • fused-ring systems
  • drug discovery
  • heterocycles

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