Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines

• DOI: 10.1016/j.ejmech.2018.05.043
• Publication Date: 2018-05-30T17:09:35Z
• Authors: Rafał Moszczyński...; Jakub Majer; Małgorzata Borkowska; Łukasz Bojarski; Sylwia Janowska; Mikołaj Matłoka; Filip Stefaniak; Damian Smuga; Katarzyna Bazydło; Krzysztof Dubiel; Maciej Wieczorek
• Keywords: PDE10A; Metabolic stability

New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.