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1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands |
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| Authors: | Park Chul Min Choi Jin Il Choi Jung Hwan Kim So Young Park Woo Kyu Seong Churl Min |
| Institution: | a Medicinal Chemistry Research Center, Bio-Organic Division, Korea Research Institute of Chemical Technology, Sinseongno 19, Yuseong-gu, Daejeon 305-600, South Korea b Energy Materials Research Center, Advanced Materials Division, Korea Research Institute of Chemical Technology, Sinseongno 19, Yuseong-gu, Daejeon 305-600, South Korea c Pharmacology Research Center, Bio-Organic Division, Korea Research Institute of Chemical Technology, Sinseongno 19, Yuseong-gu, Daejeon 305-600, South Korea |
| Abstract: | 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. |
| Keywords: | 5-HT6 receptor Antagonist Memory dysfunction Brain penetrant |
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