Fluorinated cannabinoid CB2 receptor ligands: Synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives

A series of fluorinated 2-oxo-quinoline derivatives were synthesized and their in vitro assay was performed against [3H]CP-55,940, using the human cancer cell line U87, genetically engineered to express human CB2 or CB1 receptors. Of all the synthesized compounds, six compounds displayed inhibition constant (Ki) value at the level of nanomolar and sub-nanomolar concentrations. Preliminary in vitro results suggest that these six compounds may be useful for therapeutic application to neuropathic pain, neuroinflammatory diseases and immune disorders.