Literature DB >> 15603943

Synthesis and antimalarial evaluation of new N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

Adina Ryckebusch1, Marie-Ange Debreu-Fontaine, Elisabeth Mouray, Philippe Grellier, Christian Sergheraert, Patricia Melnyk.   

Abstract

Synthesis and evaluation of the activity of new N(1)-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives against a chloroquine-resistant strain of Plasmodium falciparum are described. Selectivity indices were improved for two compounds versus the lead 1, the bis-cyclopropylmethyl derivative, thus increasing the therapeutic interest of our family. As our previous studies conducted on the mode of action of our compounds made us hypothesize the existence of original mechanisms and/or original targets, terminal amino derivatives can be considered as promising tools further mechanistical studies, as probes for affinity chromatography.

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Year:  2005        PMID: 15603943     DOI: 10.1016/j.bmcl.2004.10.080

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


  6 in total

1.  3-Halo Chloroquine Derivatives Overcome Plasmodium falciparum Chloroquine Resistance Transporter-Mediated Drug Resistance in P. falciparum.

Authors:  Sonia Edaye; Dagobert Tazoo; D Scott Bohle; Elias Georges
Journal:  Antimicrob Agents Chemother       Date:  2015-10-05       Impact factor: 5.191

2.  Growth, crystal structure, Hirshfeld surface analysis, DFT studies, physicochemical characterization, and cytotoxicity assays of novel organic triphosphate.

Authors:  Yathreb Oueslati; Sevgi Kansız; Necmi Dege; Cristina de la Torre Paredes; Antoni Llopis-Lorente; Ramón Martínez-Máñez; Wajda Smirani Sta
Journal:  J Mol Model       Date:  2022-02-19       Impact factor: 1.810

3.  Structural modifications of quinoline-based antimalarial agents: Recent developments.

Authors:  Sandhya Bawa; Suresh Kumar; Sushma Drabu; Rajiv Kumar
Journal:  J Pharm Bioallied Sci       Date:  2010-04

4.  Antimalarial activity and mechanisms of action of two novel 4-aminoquinolines against chloroquine-resistant parasites.

Authors:  Anna Caroline Campos Aguiar; Raquel de Meneses Santos; Flávio Júnior Barbosa Figueiredo; Wilian Augusto Cortopassi; André Silva Pimentel; Tanos Celmar Costa França; Mario Roberto Meneghetti; Antoniana Ursine Krettli
Journal:  PLoS One       Date:  2012-05-23       Impact factor: 3.240

5.  Anti-malarial effect of novel chloroquine derivatives as agents for the treatment of malaria.

Authors:  Seon-Ju Yeo; Dong-Xu Liu; Hak Sung Kim; Hyun Park
Journal:  Malar J       Date:  2017-02-17       Impact factor: 2.979

6.  Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.

Authors:  Irene Sola; Albert Artigas; Martin C Taylor; F Javier Pérez-Areales; Elisabet Viayna; M Victòria Clos; Belén Pérez; Colin W Wright; John M Kelly; Diego Muñoz-Torrero
Journal:  Bioorg Med Chem       Date:  2016-08-22       Impact factor: 3.641

  6 in total

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