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Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABA A -R ligands.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2017 Mar 15; Vol. 25 (6), pp. 1901-1906. Date of Electronic Publication: 2017 Feb 11. - Publication Year :
- 2017
-
Abstract
- The synthesis of a new series of 6-phenyl- and 6-benzylpyrazolo[1,5-a]pyrimidin-7(4H)-ones 2a-g and 3a-g, strictly related to derivatives with pyrazolobenzotriazine (PBT) and pyrazoloquinazoline (PQ) scaffold, was realized. The in vitro GABA <subscript>A</subscript> -receptor subtype affinity was evaluated and from preliminary pharmacological studies, compound 3g shows anxiolytic-like effect at 10-30mg/kg.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Anti-Anxiety Agents chemical synthesis
Anti-Anxiety Agents chemistry
Anti-Anxiety Agents pharmacology
Cattle
Dose-Response Relationship, Drug
Ligands
Male
Mice
Pyrimidines chemistry
Rats
Rats, Wistar
Structure-Activity Relationship
Pyrazoles chemistry
Pyrimidines chemical synthesis
Pyrimidines pharmacology
Receptors, GABA-A metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 25
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 28237554
- Full Text :
- https://doi.org/10.1016/j.bmc.2017.02.013