Literature DB >> 19433358

Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.

Kevin G Liu1, Jennifer R Lo, Thomas A Comery, Guo Ming Zhang, Jean Y Zhang, Dianne M Kowal, Deborah L Smith, Li Di, Edward H Kerns, Lee E Schechter, Albert J Robichaud.   

Abstract

Cognitive dysfunction is a characteristic of various forms of dementia such as Alzheimer's disease (AD) and a core feature of schizophrenia. As part of our continuing efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor-one of the emerging therapeutic targets in this area. Herein, we report the identification of a novel series of 3-piperidinyl-5-sulfonylindazole derivatives as potent 5-HT(6) antagonists. The synthesis and SAR of this class of compounds are reported.

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Year:  2009        PMID: 19433358     DOI: 10.1016/j.bmcl.2009.04.108

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


  3 in total

1.  Investigation of the structure requirement for 5-HT₆ binding affinity of arylsulfonyl derivatives: a computational study.

Authors:  Ming Hao; Yan Li; Hanqing Li; Shuwei Zhang
Journal:  Int J Mol Sci       Date:  2011-08-08       Impact factor: 5.923

2.  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.  Synthesis and Antibacterial Activity of Benzo[4,5]isothiazolo[2,3-a]pyrazine-6,6-dioxide Derivatives.

Authors:  Jatinder P Bassin; Michelle J Botha; Rajesh Garikipati; Madhu Goyal; Lee Martin; Amit Shah
Journal:  Molecules       Date:  2017-11-04       Impact factor: 4.411

  3 in total

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