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 Neudorfer; Karem Shanab; Andreas Jurik; Veronika Schreiber; Carolina Neudorfer; Chrysoula Vraka; Eva Schirmer; Wolfgang Holzer; Gerhard Ecker; Markus Mitterhauser; Wolfgang Wadsak; Helmut Spreitzer

doi:10.1016/j.bmcl.2014.07.085

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 Neudorfer (Corresponding author), Karem Shanab, Andreas Jurik, Veronika Schreiber, Carolina Neudorfer, Chrysoula Vraka, Eva Schirmer, Wolfgang Holzer, Gerhard Ecker, Markus Mitterhauser, Wolfgang Wadsak, Helmut Spreitzer

Publications: Contribution to journal › Article › Peer Reviewed

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.

Original language	English
Pages (from-to)	4490-4495
Number of pages	6
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	24
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2014.07.085
Publication status	Published - 15 Sept 2014

Austrian Fields of Science 2012

301207 Pharmaceutical chemistry
301305 Medical chemistry
301303 Medical biochemistry
102005 Computer aided design (CAD)

Keywords

MAO-B
Alzheimer's disease
PET
Pyrazoline derivatives
Molecular imaging
MONOAMINE-OXIDASE-B
EMPIRICAL SCORING FUNCTIONS
PROTEIN-LIGAND DOCKING
1-N-SUBSTITUTED THIOCARBAMOYL-3-PHENYL-5-THIENYL-2-PYRAZOLINES
PLATELET SEROTONIN
EXPRESSION
AUTORADIOGRAPHY
DERIVATIVES
ASTROCYTES
HYDRAZINES

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Neudorfer, C., Shanab, K., Jurik, A., Schreiber, V., Neudorfer, C., Vraka, C., Schirmer, E., Holzer, W., Ecker, G., Mitterhauser, M., Wadsak, W., & Spreitzer, H. (2014). 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. Bioorganic & Medicinal Chemistry Letters, 24(18), 4490-4495. https://doi.org/10.1016/j.bmcl.2014.07.085

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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.",

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author = "Catharina Neudorfer and Karem Shanab and Andreas Jurik and Veronika Schreiber and Carolina Neudorfer and Chrysoula Vraka and Eva Schirmer and Wolfgang Holzer and Gerhard Ecker and Markus Mitterhauser and Wolfgang Wadsak and Helmut Spreitzer",

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doi = "10.1016/j.bmcl.2014.07.085",

language = "English",

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journal = "Bioorganic & Medicinal Chemistry Letters",

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Neudorfer, C, Shanab, K, Jurik, A, Schreiber, V, Neudorfer, C, Vraka, C, Schirmer, E, Holzer, W, Ecker, G, Mitterhauser, M, Wadsak, W & Spreitzer, H 2014, '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', Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 18, pp. 4490-4495. https://doi.org/10.1016/j.bmcl.2014.07.085

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. / Neudorfer, Catharina (Corresponding author); Shanab, Karem; Jurik, Andreas et al.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 24, No. 18, 15.09.2014, p. 4490-4495.

Publications: Contribution to journal › Article › Peer Reviewed

TY - JOUR

T1 - 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

AU - Neudorfer, Catharina

AU - Shanab, Karem

AU - Jurik, Andreas

AU - Schreiber, Veronika

AU - Neudorfer, Carolina

AU - Vraka, Chrysoula

AU - Schirmer, Eva

AU - Holzer, Wolfgang

AU - Ecker, Gerhard

AU - Mitterhauser, Markus

AU - Wadsak, Wolfgang

AU - Spreitzer, Helmut

PY - 2014/9/15

Y1 - 2014/9/15

N2 - 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.

AB - 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.

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KW - Alzheimer's disease

KW - PET

KW - Pyrazoline derivatives

KW - Molecular imaging

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KW - PROTEIN-LIGAND DOCKING

KW - 1-N-SUBSTITUTED THIOCARBAMOYL-3-PHENYL-5-THIENYL-2-PYRAZOLINES

KW - PLATELET SEROTONIN

KW - EXPRESSION

KW - AUTORADIOGRAPHY

KW - DERIVATIVES

KW - ASTROCYTES

KW - HYDRAZINES

UR - http://www.scopus.com/inward/record.url?scp=84906964183&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2014.07.085

DO - 10.1016/j.bmcl.2014.07.085

M3 - Article

C2 - 25127869

SN - 0960-894X

VL - 24

SP - 4490

EP - 4495

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 18

ER -

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

Austrian Fields of Science 2012

Keywords

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