Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia

SW Yang, J Smotryski, WT McElroy, Z Tan, G Ho…

文献索引：Yang, Shu-Wei; Smotryski, Jennifer; McElroy, William T.; Tan, Zheng; Ho, Ginny; Tulshian, Deen; Greenlee, William J.; Guzzi, Mario; Zhang, Xiaoping; Mullins, Deborra; Xiao, Li; Hruza, Alan; Chan, Tze-Ming; Rindgen, Diane; Bleickardt, Carina; Hodgson, Robert Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 235 - 239

全文：HTML全文

被引用次数: 29

摘要

A series of pyrazoloquinoline analogs have been synthesized and shown to bind to PDE10 with high affinity. From the SAR study and our lead optimization efforts, compounds 16 and 27 were found to possess potent oral antipsychotic activity in the MK-801 induced hyperactive rat model.