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

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...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2017-01, Vol.22 (1), p.77
Main Authors: Moldovan, Rareş-Petru, Deuther-Conrad, Winnie, Horti, Andrew G, Brust, Peter
Format: Article
Language:English
Subjects:
Acetamides - chemical synthesis
Acetamides - pharmacology
Alzheimer's disease
Animals
binding affinity
Biomarkers
cannabinoid receptor type 2
Cannabinoid receptors
Cannabinoids
Cell Membrane - drug effects
Cell Membrane - metabolism
Chloride
CHO Cells
Communication
Contrast Media - chemical synthesis
Cricetulus
Fluorine
Gene Expression
Halogenation
Humans
Immune system
indole
Indoles - chemical synthesis
Indoles - pharmacology
Investigations
Ligands
Medical imaging
Metabolism
Neurogenesis
Pharmaceutical sciences
Positron-Emission Tomography
Protein Binding
Reagents
Receptor, Cannabinoid, CB2 - agonists
Receptor, Cannabinoid, CB2 - genetics
Receptor, Cannabinoid, CB2 - metabolism
Stereoisomerism
Structure-Activity Relationship
Transgenes
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Description
Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules22010077