Discovery Of Novel N-1 Substituted Pyrazolopyrimidinones As Potent, Selective Pde2 Inhibitors

Gregori J Morriello,Michael P Dwyer,Yili Chen, Anthony T Ginetti, Shimin Xu,Jun Lu,Pravien Abeywickrema,Deping Wang,Alejandro Crespo,Tamara D Cabalu,Jonathan E Wilson,Shawn J Stachel,Daniel V Paone,Christopher Sinz

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2021）

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摘要

A focused SAR study was conducted on a series of N1-substituted pyrazolopyrimidinone PDE2 inhibitors to reveal compounds with excellent potency and selectivity. The series was derived from previously identified internal leads and designed to enhance steric interactions with key amino acids in the PDE2 binding pocket. Compound 26 was identified as a lead compound with excellent PDE2 selectivity and good physicochemical properties.

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关键词

PDE2, cAMP, cGMP, Pyrazolopyrimidinone

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