Bioorganic & Medicinal Chemistry Letters · 2018 · 11 citations · 22 references
PharmacyChemistryMedicinal ChemistryDrug DesignDrug DiscoveryLead OptimizationChemical Library DesignCombinatorial SynthesisDiversity-oriented SynthesisFragment-based Drug DesignFragment-based Lead DiscoveryFragment-based OptimizationDiversity-oriented Library DesignFragment OptimizationFragment-based DiscoveryFragment-based Library ConstructionFragment-based Ligand DesignFragment-based Scaffold DesignPrivileged Scaffold LibrariesScaffold-based Library Synthesis
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.
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