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Literature DB >> 21093272

Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.

Kevin G Liu¹, Albert J Robichaud, Alexander A Greenfield, Jennifer R Lo, Cristina Grosanu, James F Mattes, Yanxuan Cai, Guo Ming Zhang, Jean Y Zhang, Dianne M Kowal, Deborah L Smith, Li Di, Edward H Kerns, Lee E Schechter, Thomas A Comery.

Abstract

As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT(6) antagonists. The synthesis and detailed SAR of this class of compounds are reported.

Entities: Chemical Gene

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Year: 2010 PMID： 21093272 DOI： 10.1016/j.bmc.2010.10.033

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

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Cited

5 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

Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.

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

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

3. 6,6'-Di-nitro-1,1'-(ethane-1,2-di-yl)di(1H-indazole).

4. Crystal structure of 3-chloro-1-methyl-5-nitro-1H-indazole.

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

Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.

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

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

3. 6,6'-Di-nitro-1,1'-(ethane-1,2-di-yl)di(1H-indazole).

4. Crystal structure of 3-chloro-1-methyl-5-nitro-1H-indazole.

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

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