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
- PMID: 25127869
- 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
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.
Keywords: Alzheimer’s disease; MAO-B; Molecular imaging; PET; Pyrazoline derivatives.
Copyright © 2014 Elsevier Ltd. All rights reserved.
Similar articles
-
Evaluation of nitrocatechol chalcone and pyrazoline derivatives as inhibitors of catechol-O-methyltransferase and monoamine oxidase.Bioorg Med Chem Lett. 2020 Jun 15;30(12):127188. doi: 10.1016/j.bmcl.2020.127188. Epub 2020 Apr 11. Bioorg Med Chem Lett. 2020. PMID: 32299731
-
Synthesis of some novel hydrazone and 2-pyrazoline derivatives: monoamine oxidase inhibitory activities and docking studies.Bioorg Med Chem Lett. 2014 Aug 1;24(15):3278-84. doi: 10.1016/j.bmcl.2014.06.015. Epub 2014 Jun 17. Bioorg Med Chem Lett. 2014. PMID: 24986657
-
Monoamine oxidase inhibitory activity of 3,5-biaryl-4,5-dihydro-1H-pyrazole-1-carboxylate derivatives.Eur J Med Chem. 2013 Nov;69:762-7. doi: 10.1016/j.ejmech.2013.09.010. Epub 2013 Sep 18. Eur J Med Chem. 2013. PMID: 24099995
-
Pyrazoline Derivatives as Promising MAO-A Targeting Antidepressants: An Update.Curr Top Med Chem. 2024;24(5):401-415. doi: 10.2174/0115680266280249240126052505. Curr Top Med Chem. 2024. PMID: 38318823 Review.
-
Synthesis, biological evaluation and 3D-QSAR of 1,3,5-trisubstituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase A inhibitors.Curr Med Chem. 2006;13(12):1411-28. doi: 10.2174/092986706776872907. Curr Med Chem. 2006. PMID: 16719786 Review.
Cited by
-
1-[5-(3,5-Di-meth-oxy-phen-yl)-3-(2-meth-oxy-phen-yl)-4,5-di-hydro-1H-pyrazol-1-yl]ethanone.IUCrdata. 2021 Jan 29;6(Pt 1):x210096. doi: 10.1107/S2414314621000961. eCollection 2021 Jan. IUCrdata. 2021. PMID: 36340475 Free PMC article.
-
Pyrazoline Containing Compounds as Therapeutic Targets for Neurodegenerative Disorders.ACS Omega. 2022 Oct 17;7(43):38207-38245. doi: 10.1021/acsomega.2c05339. eCollection 2022 Nov 1. ACS Omega. 2022. PMID: 36340076 Free PMC article. Review.
-
Crystal structure of 3-meth-oxy-2-[5-(naphthalen-1-yl)-4,5-di-hydro-1H-pyrazol-3-yl]phenol.Acta Crystallogr E Crystallogr Commun. 2015 Oct 7;71(Pt 11):o828-9. doi: 10.1107/S2056989015018472. eCollection 2015 Nov 1. Acta Crystallogr E Crystallogr Commun. 2015. PMID: 26594549 Free PMC article.
-
Crystal structure of 3,5-dimeth-oxy-2-[5-(naphthalen-1-yl)-4,5-di-hydro-1H-pyrazol-3-yl]phenol.Acta Crystallogr E Crystallogr Commun. 2015 Sep 12;71(Pt 10):o708-9. doi: 10.1107/S2056989015016369. eCollection 2015 Oct 1. Acta Crystallogr E Crystallogr Commun. 2015. PMID: 26594435 Free PMC article.
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources
Medical