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The SAR Development of Dihydroimidazoisoquinoline Derivatives as Phosphodiesterase 10A Inhibitors for the Treatment of Schizophrenia

Ginny D Ho, W Michael Seganish, Ana Bercovici, Deen Tulshian, William J Greenlee, Rachel Van Rijn, Alan Hruza, Li Xiao, Diane Rindgen, Deborra Mullins, Mario Guzzi, Xiaoping Zhang, Carina Bleickardt, Robert Hodgson

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2585-9.

PMID: 22377514

Abstract:

The identification of potent and orally active dihydroimidazoisoquinolines as PDE 10A inhibitors is reported. The SAR development led to the discovery of compound 35 as a potent, selective, and orally active PDE10A inhibitor. Compound 35 inhibited MK-801-induced hyperactivity at 3mg/kg and displayed a 10-fold separation between the minimal effective doses for inhibition of MK-801-induced hyperactivity and hypolocomotion in rats.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR4245724 PDE7A active rat PDE7A active rat Price
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