The derivatization of resin-bound aminobenzimidazole toward the parallel solid-phase synthesis of aminobenzimidazole tethered pharmacologically important heterocycles such as quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines is reported. All the compounds were tested for IKK inhibition. Only one compound elicited significant inhibition of IKKε, TBK-1 and IKK2.
Keywords: 1,3-Dipolar cycloaddition; Aminobenzimidazoles; Benzodiazepinetriones; Heterocycles; Intramolecular cyclization; Isoxazoles; Isoxazolines; Quinazolinediones; Solid-phase synthesis; Thioxoquina-zolinones.
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