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
- Author(s)
- Catharina Neudorfer, Karem Shanab, Andreas Jurik, Veronika Schreiber, Carolina Neudorfer, Chrysoula Vraka, Eva Schirmer, Wolfgang Holzer, Gerhard Ecker, Markus Mitterhauser, Wolfgang Wadsak, Helmut Spreitzer
- 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.
- Organisation(s)
- Department of Nutritional Sciences, Department of Inorganic Chemistry
- External organisation(s)
- Medizinische Universität Wien
- Journal
- Bioorganic & Medicinal Chemistry Letters
- Volume
- 24
- Pages
- 4490-4495
- No. of pages
- 6
- ISSN
- 0960-894X
- DOI
- https://doi.org/10.1016/j.bmcl.2014.07.085
- Publication date
- 09-2014
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 301207 Pharmaceutical chemistry, 301305 Medical chemistry, 301303 Medical biochemistry, 102005 Computer aided design (CAD)
- Keywords
- ASJC Scopus subject areas
- Drug Discovery, Molecular Medicine, Molecular Biology, Biochemistry, Clinical Biochemistry, Pharmaceutical Science, Organic Chemistry
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/ac413845-9a81-4e24-8ea8-494374785153