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ID: ALA4152287

Journal: Eur J Med Chem

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

Authors: Moszczyński-Pętkowski R, Majer J, Borkowska M, Bojarski Ł, Janowska S, Matłoka M, Stefaniak F, Smuga D, Bazydło K, Dubiel K, Wieczorek M.

Abstract: 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.

CiteXplore: 29870883

DOI: 10.1016/j.ejmech.2018.05.043