1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT 6 serotonin receptor ligands

Article abstract of DOI:10.1016/j.bmcl.2010.12.007

Piperazinyl derivatives of 1-(arylsulfonyl)-2,3-dihydro-1H-quinolin-4-ones have been identified with high binding affinities for 5-HT₆ receptor. In particular, 2-methyl-5-(N-methyl-piperazin-1-yl)-1-(naphthalene-2-sulfonyl)- 2,3-dihydro-1H-quinolin-4-one (8g) exhibits high binding affinity toward 5-HT₆ (IC₅₀ = 8 nM) receptor with good selectivity over other serotonin and dopamine receptors.