Literature DB >> 25127869

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.

Catharina Neudorfer1, Karem Shanab2, Andreas Jurik3, Veronika Schreiber4, Carolina Neudorfer5, Chrysoula Vraka6, Eva Schirmer5, Wolfgang Holzer5, Gerhard Ecker3, Markus Mitterhauser7, Wolfgang Wadsak7, Helmut Spreitzer8.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Alzheimer’s disease; MAO-B; Molecular imaging; PET; Pyrazoline derivatives

Mesh:

Substances:

Year:  2014        PMID: 25127869     DOI: 10.1016/j.bmcl.2014.07.085

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.940


  2 in total

1.  Crystal structure of 3,5-dimeth-oxy-2-[5-(naphthalen-1-yl)-4,5-di-hydro-1H-pyrazol-3-yl]phenol.

Authors:  Dongsoo Koh
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-09-12

2.  Crystal structure of 3-meth-oxy-2-[5-(naphthalen-1-yl)-4,5-di-hydro-1H-pyrazol-3-yl]phenol.

Authors:  Dongsoo Koh
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-10-07
  2 in total

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