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      https://www.ias.ac.in/article/fulltext/jcsc/127/03/0439-0445

    • Keywords

       

      [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indoles; 5-HT6R antagonists; cognitive impairment; structure activity relationship; cross selectivity; pharmacokinetic profile.

    • Abstract

       

      In continuation to our efforts to develop better treatment options for cognitive decline, we have been focussing on 5-HT6 receptor (5-HT6R) antagonists, which are known to be involved in improving cognitive function in numerous animal models. In this paper, we report a novel series of [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives as potent and selective 5-HT6R antagonists. The lead compound from this series shows potent in vitro binding affinity, functional antagonistic activity at 5-HT6R, good pharmacokinetic profile, excellent selectivity and no Cytochrome P450 liabilities.

    • Author Affiliations

       

      Ramakrishna V S Nirogi1 Rajesh Kumar Badange1 2 Kiran Kumar Kandukuri1 Mukkanti Khagga2

      1. Discovery Research, Suven Life Sciences Limited, Serene Chambers, Road 5, Avenue 7, Banjara Hills, Hyderabad 500 034, India
      2. Institute of Science and Technology, JNTU Hyderabad, Kukatpally, Hyderabad 500 085, India
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    • Supplementary Material

       
  • Journal of Chemical Sciences | News

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