Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound

DOI: 10.1016/j.bmcl.2011.12.080

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1335 - 1339 (2012)

Update date:2022-08-05

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Authors:

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

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Article abstract of DOI:10.1016/j.bmcl.2011.12.080

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 10 mg/kg in an in vivo model.

Full text of DOI:10.1016/j.bmcl.2011.12.080

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