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Molecules 2017, 22(1), 77; doi:10.3390/molecules22010077

Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands

1
Helmholtz-Zentrum Dresden-Rossendorf e.V., Institute of Radiopharmaceutical Cancer Research, Permoserstr. 15, 04318 Leipzig, Germany
2
Johns Hopkins School of Medicine, Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Baltimore, MD 21287, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 21 October 2016 / Revised: 22 December 2016 / Accepted: 22 December 2016 / Published: 4 January 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [527 KB, uploaded 4 January 2017]   |  

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. View Full-Text
Keywords: positron emission tomography; cannabinoid receptor type 2; binding affinity; indole positron emission tomography; cannabinoid receptor type 2; binding affinity; indole
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Moldovan, R.-P.; Deuther-Conrad, W.; Horti, A.G.; Brust, P. Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands. Molecules 2017, 22, 77.

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