Literature DB >> 20932009

5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.

Kevin G Liu1, Albert J Robichaud, Ronald C Bernotas, Yinfa Yan, Jennifer R Lo, Mei-Yi Zhang, Zoe A Hughes, Christine Huselton, Guo Ming Zhang, Jean Y Zhang, Dianne M Kowal, Deborah L Smith, Lee E Schechter, Thomas A Comery.   

Abstract

As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-HT(6) antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.

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Year:  2010        PMID: 20932009     DOI: 10.1021/jm1007825

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Metal- and base-free tandem sulfonylation/cyclization of 1,5-dienes with aryldiazonium salts via the insertion of sulfur dioxide.

Authors:  Xiaohong Wang; Fengzhi You; Baojian Xiong; Lei Chen; Xuemei Zhang; Zhong Lian
Journal:  RSC Adv       Date:  2022-06-06       Impact factor: 4.036

2.  Synthesis and biological evaluation against Leishmania donovani of novel hybrid molecules containing indazole-based 2-pyrone scaffolds.

Authors:  M El Ghozlani; L Bouissane; M Berkani; S Mojahidi; A Allam; C Menendez; S Cojean; P M Loiseau; M Baltas; E M Rakib
Journal:  Medchemcomm       Date:  2018-11-19       Impact factor: 3.597

3.  Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Authors:  Haizhou Zhu; Venkateshwara Dronamraju; Wei Xie; Swati S More
Journal:  Med Chem Res       Date:  2021-01-15       Impact factor: 1.965

  3 in total

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