Group Prof. Briel

 

 

 

Prof. Dr. Detlef Briel

Syntheses of Annulated Heterocycles as Inhibitors of PDE 2A & 10A

The phosphodiesterase (PDE) are enzymes which hydrolyze the two cellular messengers cyclic adenosine monophoshate (cAMP) and cyclic guanosine monophosphate (cGMP). Through the functioning of these on cellular signaling cascades and self-regulation (homeostasis) basic functions such as behavior, learning, memory and recognition are controlled and mental illness are affected. The local distribution and function of PDE2A makes molecular imaging by positron emission tomography (PET) promising regarding a better understanding of disorders in humans that are correlated with related diseases.

Aim of the project is the synthesis of triazole based tricyclic compounds as potential precursors for 18F-labeled radiotracers for PDE2A in vivo.

Cooperation with

Prof. Dr. Peter Brust link
Institute of Radiopharmacy, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf

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Syntheses Quinazoline Derivates as Adenosine A3 Receptor Antagonists

The nucleaside adenosine (ADO) as an extracellular signaling molecule triggers distinct cell reactions. It can spread its effects via G-protein coupled adenosine receptors (ADOR), which are sectioned in four subtypes: A1, A2a, A2b and A3. Apparently this receptor might be involved in progression of several inflammatory diseases, as for instace asthma bronchiale, COPD or IPF. Moreover, ADORA3 antagonists may be useful for the treatment of cancer. Our aim is to synthezise substituted quinazolines to find potent and selective ADORA3-Antagonist.

Cooperation with

Prof. Dr. Christa E. Müller
(Fachgruppe Pharmazie; Rheinische Friedrich-Wilhelms-Universität Bonn)

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Development of tricyclic PDE2A-Inhibitors and their use as PET-Radiotracer

This project aims the development of new drugs or diagnostics, which are important for the detection and treatment of neurodegenerative diseases, like alzheimer´s dementia, depression and anxiety disorders.

The work includes the synthesis and characterization of PDE2A enzyme inhibitors. Decisive for further development as a radiotracer is a high potency as well as a high selectivity against the target enzyme PDE2A.

The project is a collaborative effort between the Institute of Pharmacy (department of pharm. med. chemistry, working group Prof. Briel: synthesis of tricyclic heterocycles, test of potency, chemical and metabolic stability and structure effects) and the Helmholtz-Zentrum Dresden Rossendorf (HZDR, working group Dr. Scheunemann: radiomarking, in vitro and in vivo testing of radiotracers).

Cooperation with

Prof. Dr. Peter Brust link
Institute of Radiopharmacy, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf

Prof. Dr. Osama Sabri link
Clinic for Nuclear Medicine, Universtiy of Leipzig

Prof. Dr. Jörg Matysik & Dr. Claudia Birkemeyer
faculty of Chemistry and Mineralogy, University of Leipzig

AG Prof. Huang
PET-center at the Yale university New Haven, USA

The project is funded by the DFG.

last modified: 13.03.2017