Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound

…, D Tulshian, WJ Greenlee, D Mullins, M Guzzi…

Index: McElroy, William T.; Tan, Zheng; Basu, Kallol; Yang, Shu-Wei; Smotryski, Jennifer; Ho, Ginny D.; Tulshian, Deen; Greenlee, William J.; Mullins, Deborra; Guzzi, Mario; Zhang, Xiaoping; Bleickardt, Carina; Hodgson, Robert Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 3 p. 1335 - 1339

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Citation Number: 22

Abstract

A series of pyrazoloquinolines, possessing (hetero) arylhydroxymethyl substituents at the quinoline C-4 position were evaluated as PDE10A inhibitors. Among these, methylpyrimidyl analogue 15 was identified as having good rodent and monkey exposure, and a MED of 10mg/kg in an in vivo model.