| Literature DB >> 33991626 |
Gregori J Morriello1, Michael P Dwyer2, Yili Chen2, Anthony T Ginetti2, Shimin Xu2, Jun Lu3, Pravien Abeywickrema3, Deping Wang3, Alejandro Crespo3, Tamara D Cabalu4, Jonathan E Wilson3, Shawn J Stachel3, Daniel V Paone3, Christopher Sinz5.
Abstract
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.Entities:
Keywords: PDE2; Pyrazolopyrimidinone; cAMP; cGMP
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Year: 2021 PMID： 33991626 DOI： 10.1016/j.bmcl.2021.128082
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823