Abstract：
:Substituted diphenyl sulfones (10a-n) were synthesised, and the structures were confirmed by NMR, LC-MS and X-ray crystallography. Their antagonistic activities towards 5-HT₆ receptor were assessed in a cell-based functional assay. Diphenyl sulfone 10a, in spite of being the smallest and simplest known sulfonyl-containing 5-HT₆R antagonist, showed a strong potency (Ki=1.6 μM). Its derivative with a methylamine substituent, 10g (N-methyl-2-(phenylsulfonyl)aniline), was ∼66-times as active as diphenyl sulfone (Ki=24.3 nM). Addition of a piperazinyl moiety in the para-position relative to the sulfonyl group in compound 10m (N-methyl-2-(phenylsulfonyl)-5-piperazin-1-ylaniline) led to a further 150-fold increase in potency (Ki=0.16 nM) to block the serotonin-induced response of HEK-293 cells that were stably transfected with the human recombinant 5-HT₆ receptor.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Ivachtchenko A,Golovina E,Kadieva M,Mitkin O,Tkachenko S,Okun Idoi
10.1016/j.bmc.2013.05.040subject
Has Abstractpub_date
2013-08-01 00:00:00pages
4614-27issue
15eissn
0968-0896issn
1464-3391pii
S0968-0896(13)00489-6journal_volume
21pub_type
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