Diversity-oriented synthesis of bicyclic fragments containing privileged azines

Nicola Luise, Paul G. Wyatt (Lead / Corresponding author)

Research output: Contribution to journalArticle

2 Citations (Scopus)
152 Downloads (Pure)

Abstract

An innovative and efficient reagent- and scaffold-based diversity oriented synthesis (DOS) of a fragment set was developed for fragment-based drug discovery (FBDD) programs. Twelve diverse, functionalized and bicyclic scaffolds were rapidly accessed by adopting a convenient synthetic toolkit around three privileged azine cores in order to effectively modulate biomolecules. These structures are characterized by both key motifs for interacting with diverse biological targets via hydrogen bonds and useful points of growth for subsequent fragment optimization.
Original languageEnglish
Pages (from-to)248-251
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume29
Issue number2
Early online date24 Nov 2018
DOIs
Publication statusPublished - 15 Jan 2019

Keywords

  • Diversity-oriented synthesis
  • Drug discovery
  • Fused-ring system
  • Heterocycles
  • Synthetic methods

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