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

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]}

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

• 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