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Bioorg Med Chem Lett. 2011 Jan 15;21(2):698-703. doi: 10.1016/j.bmcl.2010.12.007. Epub 2010 Dec 8.

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

Author information

1
Medicinal Chemistry Research Center, Bio-Organic Division, Korea Research Institute of Chemical Technology, Sinseongno 19, Yuseong-gu, Daejeon 305-600, South Korea. parkcm@krict.re.kr

Abstract

Piperazinyl derivatives of 1-(arylsulfonyl)-2,3-dihydro-1H-quinolin-4-ones have been identified with high binding affinities for 5-HT(6) 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-HT(6) (IC(50)=8nM) receptor with good selectivity over other serotonin and dopamine receptors.

PMID:
21190848
DOI:
10.1016/j.bmcl.2010.12.007
[Indexed for MEDLINE]

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