吲哚-3-基-氧代乙酰胺作为强效大麻素受体2型配体的合成及初步生物学评价
Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands.
作者信息
Moldovan Rareş-Petru, Deuther-Conrad Winnie, Horti Andrew G, Brust Peter
机构信息
Helmholtz-Zentrum Dresden-Rossendorf e.V., Institute of Radiopharmaceutical Cancer Research, Permoserstr. 15, 04318 Leipzig, Germany.
Johns Hopkins School of Medicine, Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Baltimore, MD 21287, USA.
出版信息
Molecules. 2017 Jan 4;22(1):77. doi: 10.3390/molecules22010077.
A small series of indol-3-yl-oxoacetamides was synthesized starting from the literature known -(adamantan-1-yl)-2-(5-(furan-2-yl)-1-pentyl-1-indol-3-yl)-2-oxoacetamide () by substituting the 1-pentyl-1-indole subunit. Our preliminary biological evaluation showed that the fluorinated derivative 8 is a potent and selective CB₂ ligand with = 6.2 nM.
从文献中已知的-(金刚烷-1-基)-2-(5-(呋喃-2-基)-1-戊基-1-吲哚-3-基)-2-氧代乙酰胺()开始，通过取代1-戊基-1-吲哚亚基，合成了一小系列吲哚-3-基-氧代乙酰胺。我们的初步生物学评估表明，氟化衍生物8是一种有效的选择性CB₂配体，IC₅₀ = 6.2 nM。
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