Literature DB >> 17588750

Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.

María Barceló1, Enrique Raviña, Christian F Masaguer, Eduardo Domínguez, Filipe Miguel Areias, José Brea, María I Loza.   

Abstract

We describe the synthesis and binding affinities on D(2), 5-HT(2A) and 5-HT(2C) receptors of 6-aminomethyl-6,7-dihydro-1H-indazol-4(5H)-ones and 6-aminomethyl-6,7-dihydro-3-methyl-benzo[d]isoxazol-4(5H)-ones, as conformationally constrained butyrophenone analogues. One of the new compounds showed good in vitro binding features, and a Meltzer's ratio characteristic of an atypical antipsychotic profile.

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Year:  2007        PMID： 17588750     DOI： 10.1016/j.bmcl.2007.06.045

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


  7 in total

1.  Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi.

Authors:  Julianna Siciliano de Araújo; Cristiane França da Silva; Denise da Gama Jaén Batista; Aline Nefertiti; Ludmila Ferreira de Almeida Fiuza; Cristina Rosa Fonseca-Berzal; Patrícia Bernardino da Silva; Marcos Meuser Batista; Maarten Sijm; Titilola D Kalejaiye; Harry P de Koning; Louis Maes; Geert Jan Sterk; Rob Leurs; Maria de Nazaré Correia Soeiro
Journal:  Antimicrob Agents Chemother       Date:  2020-08-20       Impact factor: 5.191

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

3.  Efficient one-pot protocol for diverse pyrazolylphosphonates by multi-component reactions: their antioxidant and antibacterial activities.

Authors:  So Rang Kang; Yong Rok Lee
Journal:  Mol Divers       Date:  2015-02-05       Impact factor: 2.943

4.  Synthesis of thiazolo- and 7,8-dihydrothiazolo[4,5-e]benzoisoxazoles.

Authors:  M H El-Badri; Mark J Kurth
Journal:  J Comb Chem       Date:  2009-03-09

5.  Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]pyrazole and pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidine derivatives.

Authors:  Mohamed A M Abdel Reheim; Safaa M Baker
Journal:  Chem Cent J       Date:  2017-11-02       Impact factor: 4.215

6.  Ethyl 5-(4-amino-phen-yl)isoxazole-3-carboxyl-ate.

Authors:  Jun-Tao Zhao; Jing-Jing Qi; You-Jun Zhou; Jia-Guo Lv; Ju Zhu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-17

7.  Identification of a Potent Cytotoxic Pyrazole with Anti-Breast Cancer Activity That Alters Multiple Pathways.

Authors:  Denisse A Gutierrez; Lisett Contreras; Paulina J Villanueva; Edgar A Borrego; Karla Morán-Santibañez; Jessica D Hess; Rebecca DeJesus; Manuel Larragoity; Ana P Betancourt; Jonathon E Mohl; Elisa Robles-Escajeda; Khodeza Begum; Sourav Roy; Robert A Kirken; Armando Varela-Ramirez; Renato J Aguilera
Journal:  Cells       Date:  2022-01-12       Impact factor: 6.600
  7 in total

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