| Full text | |
| Author(s): Show less - |
Wagner, Stefan
[1]
;
Gatti, Fernando de Moura
[2, 3]
;
Silva, Daniel G.
[4]
;
Zacarias, Natalia V. Ortiz
[5]
;
Zweemer, Annelien J. M.
[5]
;
Hermann, Sven
[4]
;
De Maria, Monica
[6]
;
Koch, Michael
[7]
;
Weiss, Christina
[7]
;
Schepmann, Dirk
[2]
;
Heitman, Laura H.
[5]
;
Tschammer, Nuska
[8]
;
Kopka, Klaus
[9, 10]
;
Junker, Anna
[2, 4]
Total Authors: 14
|
| Affiliation: | [1] Univ Hosp Munster, Dept Nucl Med, Albert Schweitzer Campus 1, Bldg A1, D-48149 Munster - Germany
[2] Univ Munster, Inst Pharmazeut & Med Chem, Corrensstr 48, D-48149 Munster - Germany
[3] Univ Sao Paulo, Fac Ciencias Farmaceut, Av Prof Lineu Prestes 580, BR-05508900 Sao Paulo, SP - Brazil
[4] European Inst Mol Imaging EIMI, Waldeyerstr 15, D-48149 Munster - Germany
[5] Leiden Univ, Leiden Acad Ctr Drug Res LACDR, Einsteinweg 55, NL-2333 CC Leiden - Netherlands
[6] Friedrich Alexander Univ, Dept Dev Biol, Staudtstr 5, D-91058 Erlangen - Germany
[7] Bayer AG, Res & Dev Lead Discovery Wuppertal, Aprather Weg 18a, Gebaude 456, D-42096 Wuppertal - Germany
[8] Friedrich Alexander Univ Erlangen Nurnberg, Emil Fischer Ctr, Dept Chem & Pharm, Schuhstr 19, D-91052 Erlangen - Germany
[9] Tech Univ Dresden, Fac Chem & Food Chem, D-01062 Dresden - Germany
[10] Helmholtz Zentrum Dresden Rossendorf, Inst Radiopharmazeut Krebsforsch, Bautzner Landstr 400, D-01328 Dresden - Germany
Total Affiliations: 10
|
| Document type: | Journal article |
| Source: | CHEMMEDCHEM; v. 16, n. 4 NOV 2020. |
| Web of Science Citations: | 1 |
| Abstract | |
Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as F-18-labeled PET tracers. The derivatives were evaluated extensively for their off-target profile at 48 different targets. The most potent and selective candidate was applied in vivo in a biodistribution study, demonstrating a promising profile for further preclinical development. This compound represents the first potential nonpeptidic PET tracer for the imaging of CCR2 receptors. (AU) | |
| FAPESP's process: | 17/22001-0 - Synthesis and evaluation of new heterocyclic compounds as potential antitrypanosomal agents |
| Grantee: | Daniel Gedder Silva |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |