Discovery of imidazo [1, 5-a] pyrido [3, 2-e] pyrazines as a new class of phosphodiesterase 10A inhibitiors

…, C Grunwald, B Langen, U Egerland…

文献索引：Grunwald, Christian; Rundfeldt, Chris; Lankau, Hans-Joachim; Arnold, Thomas; Hoefgen, Norbert; Dost, Rita; Egerland, Ute; Hofmann, Hans-Joerg; Unverferth, Klaus Journal of Medicinal Chemistry, 2006 , vol. 49, # 6 p. 1855 - 1866

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被引用次数: 57

摘要

Novel imidazo [1, 5-a] pyrido [3, 2-e] pyrazines have been synthesized and characterized as both potent and selective phosphodiesterase 10A (PDE10A) inhibitors. For in vitro characterization, inhibition of PDE10A mediated cAMP hydrolysis was used and a QSAR model was established to analyze substitution effects. The outcome of this analysis was complemented by the crystal structure of PDE10A in complex with compound 49. ...