Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands
Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands
Moldovan, R.-P.; Deuther-Conrad, W.; Horti, A. G.; Brust, P.
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.
Keywords: positron emission tomography; cannabinoid receptor type 2; binding affinity; indole
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Molecules 22(2017)1, 77
DOI: 10.3390/molecules22010077
Cited 3 times in Scopus
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Permalink: https://www.hzdr.de/publications/Publ-24193