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.

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.

• Authors: Catharina Neudorfer, Karem Shanab, Andreas Jurik, Veronika Schreiber, Carolina Neudorfer, Chrysoula Vraka, Eva Schirmer, Wolfgang Holzer, Gerhard Ecker, Markus Mitterhauser, Wolfgang Wadsak, Helmut Spreitzer
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 18 Pg. 4490-4495 (Sep 15 2014) ISSN: 1464-3405 [Electronic] England
• PMID: 25127869 (Publication Type: Journal Article)
• Copyright: Copyright © 2014 Elsevier Ltd. All rights reserved.

Chemical References

• Monoamine Oxidase Inhibitors
• Pyrazoles
• Monoamine Oxidase

Topics

• Alzheimer Disease (diagnosis, enzymology, metabolism)
• Dose-Response Relationship, Drug
• Early Diagnosis
• Humans
• Molecular Structure
• Monoamine Oxidase (metabolism)
• Monoamine Oxidase Inhibitors (chemistry, pharmacology)
• Positron-Emission Tomography
• Pyrazoles (chemistry, pharmacology)
• Reference Standards
• Structure-Activity Relationship