Literature DB >> 21134749

Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists.

Ramakrishna V S Nirogi1, Amol D Deshpande, Ramasastri Kambhampati, Rajesh Kumar Badange, Laxman Kota, Anand V Daulatabad, Anil K Shinde, Ishtiyaque Ahmad, Vishwottam Kandikere, Pradeep Jayarajan, P K Dubey.   

Abstract

N(1)-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT(6) receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT(6) receptor. The compound 7a (K(i) = 3.4 nM, functional assay IC(50) = 310 nM) shows enhanced cognitive effect when tested in NORT and Morris water maze models. Synthesis, SAR and PK profile of these novel compounds constitute the subject matter of this Letter.
Copyright © 2010. Published by Elsevier Ltd.

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Year:  2010        PMID: 21134749     DOI: 10.1016/j.bmcl.2010.11.001

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


  3 in total

1.  Organocatalytic Asymmetric Domino Michael/Henry Reaction of Indolin-3-ones with o-Formyl-β-nitrostyrenes.

Authors:  Suruchi Mahajan; Pankaj Chauhan; Charles C J Loh; Server Uzungelis; Gerhard Raabe; Dieter Enders
Journal:  Synthesis (Stuttg)       Date:  2015-04-01       Impact factor: 3.157

Review 2.  Continuous Flow Synthesis of Heterocycles: A Recent Update on the Flow Synthesis of Indoles.

Authors:  Marco Colella; Leonardo Degennaro; Renzo Luisi
Journal:  Molecules       Date:  2020-07-16       Impact factor: 4.411

3.  The effect of the intramolecular C-H⋯O interactions on the conformational preferences of bis-arylsulfones - 5-HT6 receptor antagonists and beyond.

Authors:  Justyna Kalinowska-Tłuścik; Jakub Staroń; Anna Krawczuk; Stefan Mordalski; Dawid Warszycki; Grzegorz Satała; Adam S Hogendorf; Andrzej J Bojarski
Journal:  RSC Adv       Date:  2018-05-22       Impact factor: 4.036

  3 in total

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