Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

作者: Patrick R. Verhoest , Caroline Proulx-Lafrance , Michael Corman , Lois Chenard , Christopher J. Helal

DOI: 10.1021/JM9015334

关键词: BiochemistryIn vivoPhosphoric Diester HydrolasesComputational biologyChemistryPenetrant (biochemical)

摘要: By use of chemical enablement and prospective design, a novel series selective, brain penetrant PDE9A inhibitors have been identified that are capable producing in vivo elevations cGMP.

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