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Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 44:128082
- Publication Year :
- 2021
- Publisher :
- Elsevier BV, 2021.
-
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.
- Subjects :
- Models, Molecular
Steric effects
Phosphodiesterase Inhibitors
education
Clinical Biochemistry
Binding pocket
Pharmaceutical Science
Pyrimidinones
Crystallography, X-Ray
01 natural sciences
Biochemistry
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
Humans
Molecular Biology
chemistry.chemical_classification
Dose-Response Relationship, Drug
Molecular Structure
010405 organic chemistry
Chemistry
fungi
Organic Chemistry
Cyclic Nucleotide Phosphodiesterases, Type 2
Combinatorial chemistry
0104 chemical sciences
Amino acid
010404 medicinal & biomolecular chemistry
Pyrazoles
Molecular Medicine
Selectivity
Lead compound
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 44
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....33cfdd9f39e9f739df7e6d6ec5a403b0