Busca avançada
Ano de início
Entree
(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors

Texto completo
Autor(es):
Mostrar menos -
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]
Número total de Autores: 14
Afiliação do(s) autor(es):
[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
Número total de Afiliações: 10
Tipo de documento: Artigo Científico
Fonte: CHEMMEDCHEM; v. 16, n. 4 NOV 2020.
Citações Web of Science: 1
Resumo

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)

Processo FAPESP: 17/22001-0 - Síntese e avaliação de novos compostos heterociclos como potenciais agentes tripanossomicidas
Beneficiário:Daniel Gedder Silva
Linha de fomento: Bolsas no Brasil - Pós-Doutorado