Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.
Bioorganic & Medicinal Chemistry Letters(2019)
Abstract
•Novel PDE10 inhibitors.•Optimization supported by X-ray crystal structure analysis and molecular modeling.•Potent, selective, and brain penetrant.•Improved PK profile (rat): lower clearance in vivo and decreased volume of distribution (compared to WEB-3).
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Key words
Phosphodiesterase,PDE10A,WEB-3
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