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Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands.
Moldovan, Rares-Petru; Deuther-Conrad, Winnie; Horti, Andrew G; Brust, Peter.
Afiliação
  • Moldovan RP; Helmholtz-Zentrum Dresden-Rossendorf e.V., Institute of Radiopharmaceutical Cancer Research, Permoserstr. 15, 04318 Leipzig, Germany. r.moldovan@hzdr.de.
  • Deuther-Conrad W; Helmholtz-Zentrum Dresden-Rossendorf e.V., Institute of Radiopharmaceutical Cancer Research, Permoserstr. 15, 04318 Leipzig, Germany. w.deuther-conrad@hzdr.de.
  • Horti AG; Johns Hopkins School of Medicine, Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Baltimore, MD 21287, USA. ahorti1@jhmi.edu.
  • Brust P; Helmholtz-Zentrum Dresden-Rossendorf e.V., Institute of Radiopharmaceutical Cancer Research, Permoserstr. 15, 04318 Leipzig, Germany. p.brust@hzdr.de.
Molecules ; 22(1)2017 Jan 04.
Article em En | MEDLINE | ID: mdl-28054997
ABSTRACT
A small series of indol-3-yl-oxoacetamides was synthesized starting from the literature known N-(adamantan-1-yl)-2-(5-(furan-2-yl)-1-pentyl-1H-indol-3-yl)-2-oxoacetamide (5) by substituting the 1-pentyl-1H-indole subunit. Our preliminary biological evaluation showed that the fluorinated derivative 8 is a potent and selective CB2 ligand with Ki = 6.2 nM.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Membrana Celular / Receptor CB2 de Canabinoide / Indóis / Acetamidas Limite: Animals / Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Membrana Celular / Receptor CB2 de Canabinoide / Indóis / Acetamidas Limite: Animals / Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article