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 language | English |
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Pages (from-to) | 248-251 |
Number of pages | 4 |
Journal | Bioorganic & Medicinal Chemistry Letters |
Volume | 29 |
Issue number | 2 |
Early online date | 24 Nov 2018 |
DOIs | |
Publication status | Published - 15 Jan 2019 |
Keywords
- Diversity-oriented synthesis
- Drug discovery
- Fused-ring system
- Heterocycles
- Synthetic methods
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry