Literature DB >> 21469694

Novel benzo[b]thiophene derivatives as new potential antidepressants with rapid onset of action.

Luis Berrade1, Bárbara Aisa, María J Ramirez, Silvia Galiano, Salvatore Guccione, Lise Román Moltzau, Finn Olav Levy, Ferdinando Nicoletti, Giuseppe Battaglia, Gemma Molinaro, Ignacio Aldana, Antonio Monge, Silvia Perez-Silanes.   

Abstract

We report benzo[b]thiophene derivatives synthesized according to a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT(7)R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results showed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.

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Year:  2011        PMID: 21469694     DOI: 10.1021/jm2000773

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


  7 in total

1.  A one-pot successive cyclization-alkylation strategy for the synthesis of 2,3-disubstituted benzo[b]thiophenes.

Authors:  Christopher Cunningham; Matthew Cloyd; Aimee Phillips; Soha Khan; Katherine Whalen; Tanay Kesharwani
Journal:  Org Biomol Chem       Date:  2021-05-12       Impact factor: 3.876

2.  Solvent-Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines.

Authors:  Ying Fu; Jing-Yi Wang; Dong Zhang; Yu-Feng Chen; Shuang Gao; Li-Xia Zhao; Fei Ye
Journal:  Molecules       Date:  2017-09-22       Impact factor: 4.411

3.  Synthesis, docking studies and biological evaluation of benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives on 5-HT1A serotonin receptors.

Authors:  Hernán Pessoa-Mahana; Gonzalo Recabarren-Gajardo; Jenny Fiedler Temer; Gerald Zapata-Torres; C David Pessoa-Mahana; Claudio Saitz Barría; Ramiro Araya-Maturana
Journal:  Molecules       Date:  2012-02-03       Impact factor: 4.411

4.  Synthesis, X-ray crystal structure, Hirshfeld surface analysis, and molecular docking study of novel inhibitor of hepatitis B: methyl 4-fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate.

Authors:  Alexandre V Ivachtchenko; Oleg D Mitkin; Dmitry V Kravchenko; Sergiy M Kovalenko; Svitlana V Shishkina; Natalya D Bunyatyan; Irina S Konovalova; Irina G Dmitrieva; Vladimir V Ivanov; Thierry Langer
Journal:  Heliyon       Date:  2019-11-14

5.  Bis benzothiophene Schiff bases: synthesis and in silico-guided biological activity studies.

Authors:  Yasemin Ünver; Dilek ÜnlÜer; Şahin Dİrekel; Serdar DurdaĞi
Journal:  Turk J Chem       Date:  2020-08-18       Impact factor: 1.239

6.  Synthesis of Novel Tritopic Hydrazone Ligands: Spectroscopy, Biological Activity, DFT, and Molecular Docking Studies.

Authors:  Sharmin Akther Rupa; Md Rassel Moni; Md Abdul Majed Patwary; Md Mayez Mahmud; Md Aminul Haque; Jamal Uddin; S M Tareque Abedin
Journal:  Molecules       Date:  2022-03-02       Impact factor: 4.411

7.  Synthesis and Biological Evaluation of Benzo[b]thiophene Acylhydrazones as Antimicrobial Agents against Multidrug-Resistant Staphylococcus aureus.

Authors:  Thibaut Barbier; Alexia Barbry; Jérémy Magand; Cédric Badiou; Floriane Davy; Anne Baudouin; Yves Queneau; Oana Dumitrescu; Gérard Lina; Laurent Soulère
Journal:  Biomolecules       Date:  2022-01-14
  7 in total

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