Literature DB >> 17084080

Studies towards the identification of a new generation of atypical antipsychotic agents.

Vincenzo Garzya1, Ian T Forbes, Andrew D Gribble, Mike S Hadley, Andrew P Lightfoot, Andrew H Payne, Alexander B Smith, Sara E Douglas, David G Cooper, Ian G Stansfield, Malcom Meeson, Emma E Dodds, Declan N C Jones, Martyn Wood, Charlie Reavill, Carol A Scorer, Angela Worby, Graham Riley, Peter Eddershaw, Chris Ioannou, Daniele Donati, Jim J Hagan, Emiliangelo A Ratti.   

Abstract

A rational structure-activity relationship study around compound (1) is reported. The lead optimisation programme led to the identification of sulfonamide (25), a molecule combining dopamine D2/D3 receptor antagonism with serotonin 5-HT2A, 5-HT2C, 5-HT6 receptor antagonism for an effective treatment of schizophrenia. Compound (25) was shown to possess the required in vivo activity with no EPS liability.

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Year:  2006        PMID： 17084080     DOI： 10.1016/j.bmcl.2006.10.036

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


  7 in total

1.  The differential actions of clozapine and other antipsychotic drugs on the translocation of dopamine D2 receptors to the cell surface.

Authors:  Joseph M Schrader; Craig M Irving; J Christopher Octeau; Joseph A Christian; Timothy J Aballo; Dean J Kareemo; Joseph Conti; Jodi L Camberg; J Robert Lane; Jonathan A Javitch; Abraham Kovoor
Journal:  J Biol Chem       Date:  2019-01-22       Impact factor: 5.157

2.  Insights into binding modes of 5-HT2c receptor antagonists with ligand-based and receptor-based methods.

Authors:  Chunhua Lu; Fangfang Jin; Cui Li; Weihua Li; Guixia Liu; Yun Tang
Journal:  J Mol Model       Date:  2011-01-04       Impact factor: 1.810

Review 3.  The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs.

Authors:  Richard A Glennon; Uma Siripurapu; Bryan L Roth; Renata Kolanos; Mikhail L Bondarev; Donald Sikazwe; Mase Lee; Małgorzata Dukat
Journal:  Curr Top Med Chem       Date:  2010       Impact factor: 3.295

4.  Prepulse inhibition and genetic mouse models of schizophrenia.

Authors:  Susan B Powell; Xianjin Zhou; Mark A Geyer
Journal:  Behav Brain Res       Date:  2009-05-04       Impact factor: 3.332

5.  Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol.

Authors:  Noel M Paul; Michelle Taylor; Rakesh Kumar; Jeffrey R Deschamps; Robert R Luedtke; Amy Hauck Newman
Journal:  J Med Chem       Date:  2008-09-06       Impact factor: 7.446

6.  Synthesis and evaluation of a series of 2-substituted-5-thiopropylpiperazine (piperidine)-1,3,4-oxadiazoles derivatives as atypical antipsychotics.

Authors:  Yin Chen; Xiangqing Xu; Xin Liu; Minquan Yu; Bi-Feng Liu; Guisen Zhang
Journal:  PLoS One       Date:  2012-04-30       Impact factor: 3.240

7.  Aberrant Expression of Long Non-Coding RNAs in Schizophrenia Patients.

Authors:  Shengdong Chen; Xinyang Sun; Wei Niu; Lingming Kong; Mingjun He; Wanshuai Li; Aifang Zhong; Jim Lu; Liyi Zhang
Journal:  Med Sci Monit       Date:  2016-09-21
  7 in total

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