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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

Authors :
Chrysoula Vraka
Markus Mitterhauser
Veronika Schreiber
Karem Shanab
Helmut Spreitzer
Wolfgang Holzer
Catharina Neudorfer
Eva Schirmer
Carolina Neudorfer
Wolfgang Wadsak
Andreas Jurik
Gerhard F. Ecker
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.

Details

ISSN :
0960894X
Volume :
24
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....aaeec84cfdba5defe0b890246257249f