publication . Article . Other literature type . 2017

(Radio)Syntheses and in Vitro and First in Vivo Evaluation

Michael Schäfers; Sven Hermann; Stefan Wagner; Verena Hugenberg; Albert D. Windhorst; Klaus Kopka; Robert C. Schuit;
Open Access English
  • Published: 12 Jan 2017 Journal: Journal of Medicinal Chemistry, volume 60, issue 1, pages 307-321 (issn: 0022-2623, Copyright policy)
  • Country: Netherlands
Abstract
The noninvasive imaging of MMP activity in vivo could have a high impact in basic research as well as in clinical applications. This approach can be established using radiolabeled MMP inhibitors (MMPIs) as tracers for the detection of activated MMPs by means of PET. However, the complexity of diseases associated with dysregulated MMP expression necessitates the imaging of distinct MMPs or MMP subgroups to distinguish their individual role in specific diseases. To this end, selective and potent MMP-13 inhibitors based on a N,N′-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized and successfully radiolabeled with carbon-11, fluorine-18, and gallium...
Persistent Identifiers
Subjects
free text keywords: Molecular Medicine, Drug Discovery, Selective matrix metalloproteinase inhibitors, selective MMP-13 inhibitors, positron emission tomography, radiotracer, Chemistry, Basic research, In vitro, Pharmacokinetics, Matrix metalloproteinase, Noninvasive imaging, Biochemistry, Structure–activity relationship, In vivo, In Vitro Techniques
Funded by
EC| INMIND
Project
INMIND
Imaging of Neuroinflammation in Neurodegenerative Diseases
  • Funder: European Commission (EC)
  • Project Code: 278850
  • Funding stream: FP7 | SP1 | HEALTH
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