Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy
作者
VERHOEST PATRICK R; PROULXLAFRANCE CAROLINE; CORMAN MICHAEL; CHENARD LOIS; HELAL CHRISTOPHER J; HOU XINJUN; KLEIMAN ROBIN; LIU SHENPING; MARR ERIC; MENNITI FRANK S; SCHMIDT CHRISTOPHER J; VANASEFRAWLEY MICHELLE; SCHMIDT ANNE W; WILLIAMS ROBERT D; NELSON FREDERICK R; FONSECA KARI R; LIRAS SPIROS
[摘要]:By use of chemical enablement and prospective design, it novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of producing in vivo elevations of brain cGMP.