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.
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DOI:
10.3390/molecules22010077
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发表时间:
2017-01-04
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Brust P
Brust P
中科院分区:
其他
文献类型:
--
作者:
Moldovan RP;Deuther-Conrad W;Horti AG;Brust P

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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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