title: 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.affiliation: Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Waehringer Guertel 18-20, 1090 Vienna, Austria; University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry, Division of Drug Synthesis, Althanstraße 14, 1090 Vienna, Austria. Electronic address: catharina.neudorfer@gmail.com.
authors.forename: Catharina
authors.initials: C
authors.lastname: Neudorfer
authors.affiliation: Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Waehringer Guertel 18-20, 1090 Vienna, Austria; University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry, Division of Drug Synthesis, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Karem
authors.initials: K
authors.lastname: Shanab
authors.affiliation: University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry Division of Drug Design and Medicinal Chemistry, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Andreas
authors.initials: A
authors.lastname: Jurik
authors.affiliation: University of Vienna, Faculty of Life Sciences, Division of Clinical Pharmacy and Diagnostics, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Veronika
authors.initials: V
authors.lastname: Schreiber
authors.affiliation: University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry, Division of Drug Synthesis, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Carolina
authors.initials: C
authors.lastname: Neudorfer
authors.affiliation: Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Waehringer Guertel 18-20, 1090 Vienna, Austria; University of Vienna, Department of Nutritional Sciences, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Chrysoula
authors.initials: C
authors.lastname: Vraka
authors.affiliation: University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry, Division of Drug Synthesis, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Eva
authors.initials: E
authors.lastname: Schirmer
authors.affiliation: University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry, Division of Drug Synthesis, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Holzer
authors.affiliation: University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry Division of Drug Design and Medicinal Chemistry, Althanstraße 14, 1090 Vienna, Austria.
authors.forename: Gerhard
authors.initials: G
authors.lastname: Ecker
authors.affiliation: Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Waehringer Guertel 18-20, 1090 Vienna, Austria.
authors.forename: Markus
authors.initials: M
authors.lastname: Mitterhauser
authors.affiliation: Medical University of Vienna, Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Waehringer Guertel 18-20, 1090 Vienna, Austria.
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wadsak
authors.affiliation: University of Vienna, Faculty of Life Sciences, Department of Pharmaceutical Chemistry, Division of Drug Synthesis, Althanstraße 14, 1090 Vienna, Austria. Electronic address: helmut.spreitzer@univie.ac.at.
authors.forename: Helmut
authors.initials: H
authors.lastname: Spreitzer
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis* / Q000201:enzymology / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D042241:Early Diagnosis; D006801:Humans; D015394:Molecular Structure; D008995:Monoamine Oxidase / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D049268:Positron-Emission Tomography; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology; D012015:Reference Standards; D013329:Structure-Activity Relationship
chemical_list: D008996:Monoamine Oxidase Inhibitors; D011720:Pyrazoles; D008995:Monoamine Oxidase
keywords: Alzheimer’s disease; MAO-B; Molecular imaging; PET; Pyrazoline derivatives