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Development of potential selective and reversible pyrazoline based MAO-B inhibitors as MAO-B PET tracer precursors and reference substances for the early detection of Alzheimer’s disease
- Source :
- Bioorganic & Medicinal Chemistry Letters. 24:4490-4495
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- Since high MAO-B levels are present in early stages of AD, the MAO-B system can be designated as an appropriate and prospective tracer target of molecular imaging biomarkers for the detection of early AD. According to the preceding investigations of Mishra et al. the aim of this work was the development of a compound library of selective and reversible MAO-B inhibitors by performing bioisosteric modifications of the core structure of 3-(anthracen-9-yl)-5-phenyl-4,5-dihydro-1H-pyrazoles. In conclusion, 13 new pyrazoline based derivatives have been prepared, which will serve as precursor substances for future radiolabeling as well as reference compounds for the investigation of increased MAO-B levels in AD.
- Subjects :
- Monoamine Oxidase Inhibitors
Clinical Biochemistry
Pharmaceutical Science
Early detection
Pyrazoline
Pyrazoline derivatives
Biochemistry
Structure-Activity Relationship
chemistry.chemical_compound
Alzheimer Disease
Drug Discovery
Humans
Pet tracer
Monoamine Oxidase
Molecular Biology
Dose-Response Relationship, Drug
Molecular Structure
Organic Chemistry
Reference Standards
Early Diagnosis
chemistry
Positron-Emission Tomography
Pyrazoles
Molecular Medicine
Monoamine oxidase B
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....aaeec84cfdba5defe0b890246257249f