Literature DB >> 15482912

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.

Ronald Bernotas1, Steven Lenicek, Schuyler Antane, Guo Ming Zhang, Deborah Smith, Joseph Coupet, Boyd Harrison, Lee E Schechter.   

Abstract

Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT(6) receptor ligands, among which N,N-dimethyl-N-(2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl)amine 8t and N-methyl-N-(2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl)amine 8u showed high affinity for 5-HT(6) receptors with K(i)=3.7 and 5.7 nM, respectively.

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Year:  2004        PMID： 15482912     DOI： 10.1016/j.bmcl.2004.09.003

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs.

Authors:  Richard A Glennon; Uma Siripurapu; Bryan L Roth; Renata Kolanos; Mikhail L Bondarev; Donald Sikazwe; Mase Lee; Małgorzata Dukat
Journal:  Curr Top Med Chem       Date:  2010       Impact factor: 3.295

2.  Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.

Authors:  Monika Marcinkowska; Adam Bucki; Joanna Sniecikowska; Agnieszka Zagórska; Nikola Fajkis-Zajączkowska; Agata Siwek; Monika Gluch-Lutwin; Paweł Żmudzki; Magdalena Jastrzebska-Wiesek; Anna Partyka; Anna Wesołowska; Michał Abram; Katarzyna Przejczowska-Pomierny; Agnieszka Cios; Elżbieta Wyska; Kamil Mika; Magdalena Kotańska; Paweł Mierzejewski; Marcin Kolaczkowski
Journal:  J Med Chem       Date:  2021-08-26       Impact factor: 7.446

3.  The fast and efficient KI/H2O2 mediated 2-sulfonylation of indoles and N-methylpyrrole in water.

Authors:  Jun Zhang; Zhong Wang; Lingjuan Chen; Yan Liu; Ping Liu; Bin Dai
Journal:  RSC Adv       Date:  2018-12-12       Impact factor: 4.036
  3 in total

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