Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases

Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for clinical diagnostics using non-invasive single pho...

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Autores principales: Breyholz, Hans-Jörg, Kopka, Klaus, Schäfers, Michael, Wagner, Stefan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5490406/
https://www.ncbi.nlm.nih.gov/pubmed/28556793
http://dx.doi.org/10.3390/ph10020049
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author Breyholz, Hans-Jörg
Kopka, Klaus
Schäfers, Michael
Wagner, Stefan
author_facet Breyholz, Hans-Jörg
Kopka, Klaus
Schäfers, Michael
Wagner, Stefan
author_sort Breyholz, Hans-Jörg
collection PubMed
description Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for clinical diagnostics using non-invasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. This work includes the organic chemical syntheses and in vitro evaluation of five iodinated barbiturate based MMPIs and the selection of derivative 9 for radiosyntheses of isotopologues [(123)I]9 potentially useful for MMP SPECT imaging and [(124)I]9 for MMP PET imaging.
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spelling pubmed-54904062017-07-03 Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases Breyholz, Hans-Jörg Kopka, Klaus Schäfers, Michael Wagner, Stefan Pharmaceuticals (Basel) Article Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for clinical diagnostics using non-invasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. This work includes the organic chemical syntheses and in vitro evaluation of five iodinated barbiturate based MMPIs and the selection of derivative 9 for radiosyntheses of isotopologues [(123)I]9 potentially useful for MMP SPECT imaging and [(124)I]9 for MMP PET imaging. MDPI 2017-05-30 /pmc/articles/PMC5490406/ /pubmed/28556793 http://dx.doi.org/10.3390/ph10020049 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Breyholz, Hans-Jörg
Kopka, Klaus
Schäfers, Michael
Wagner, Stefan
Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases
title Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases
title_full Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases
title_fullStr Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases
title_full_unstemmed Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases
title_short Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases
title_sort syntheses of radioiodinated pyrimidine-2,4,6-triones as potential agents for non-invasive imaging of matrix metalloproteinases
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5490406/
https://www.ncbi.nlm.nih.gov/pubmed/28556793
http://dx.doi.org/10.3390/ph10020049
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