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4-Aminoquinoline

NOT Open Access | Synthesis and in vitro antiplasmodial activity of ferrocenyl aminoquinoline derivatives

January 12, 2015 - 15:30 -- NOT Open Access
Author(s): 
Gabin Mwande Maguene, Jean-Bernard Lekana-Douki, Elisabeth Mouray, Till Bousquet, Philippe Grellier, Sylvain Pellegrini, Fousseyni Samba Toure Ndouo, Jacques Lebibi, Lydie Pélinski
Reference: 
European Journal of Medicinal Chemistry Volume 90, 27 January 2015, Pages 519–525

The aim of this study was to synthesize a series of ferrocenyl 4-aminoquinolines and to evaluate their activities against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquino-resistant).

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2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure–activity relationship and mode of action studies

May 2, 2012 - 08:46 -- Kabogo Ndegwa
Author(s): 
Kamaljit Singh, Hardeep Kaur, Kelly Chibale, Jan Balzarini, Susan Little, Prasad V. Bharatam
Reference: 
European Journal of Medicinal Chemistry, Volume 52, June 2012, Pages 82–97

MalariaWorld2-Aminopyrimidine based 4-aminoquinolines were synthesized using an efficacious protocol.

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4-aminoquinoline analogues and its platinum (II) complexes as antimalarial agents

October 19, 2011 - 14:27 -- Patrick Sampao
Author(s): 
Nicolli Bellotti de Souza, Arturene M.L. Carmo, Clarice Abramo, et al.
Reference: 
Biomedicine & Pharmacotherapy, Volume 65, Issue 4, July 2011, Pages 313-316

MalariaWorldThese compounds were tested in vivo in a murine model and revealed remarkable inhibition of parasite multiplication values, whose majority ranged from 50 to 80%. In addition they were not cytotoxic. Thus, they may be object of further research for new antimalarial agents.

Synthesis and antimalarial activities of rhenium bioorganometallics based on the 4-aminoquinoline structure

November 3, 2010 - 11:25 -- Kabogo Ndegwa
Author(s): 
Rodrigo Arancibia, Faustine Dubar, Bruno Pradines, Isabelle Forfar, Daniel Dive, A. Hugo Klahn, Christophe Biot
Reference: 
Bioorganic & Medicinal Chemistry Volume 18, Issue 22, 15 November 2010, Pages 8085-8091

A bioorganometallic approach to malaria therapy led to the discovery of ferroquine (FQ, SSR97193). To assess the importance of the electronic properties of the ferrocenyl group, cyclopentadienyltricarbonylrhenium analogues related to FQ, were synthesized.

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4-Aminoquinoline derived antimalarials: Synthesis, antiplasmodial activity and heme polymerization inhibition studies

October 13, 2010 - 10:22 -- Kabogo Ndegwa
Author(s): 
V.R. Solomon, W. Haq, M. Smilkstein, Kumkum Srivastava, Sunil K. Puri, S.B. Katti
Reference: 
European Journal of Medicinal Chemistry, Volume 45, Issue 11, November 2010, Pages 4990-4996

A new series of 4-aminoquinoline derivatives have been synthesized and found to be active against both susceptible and resistant strains of Plasmodium falciparum in vitro.

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Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline

June 14, 2010 - 12:48 -- Kabogo Ndegwa
Author(s): 
Anna Sparatore, Nicoletta Basilico, Manolo Casagrande, Silvia Parapini, Donatella Taramelli, Reto Brun, Sergio Wittlin, Fabio Sparatore
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 18, Issue 13, 1 July 2008, Pages 3737-3740

Two pyrrolizidinylalkyl derivatives of 4-amino-7-chloroquinoline (MG2 and MG3) were prepared and tested in vitro against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and in vivo in a Plasmodium berghei mouse model of infection.

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Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline–triazine conjugates

December 22, 2009 - 12:59 -- Patrick Sampao
Author(s): 
Sunny Manohar, Shabana I. Khan, Diwan S. Rawat
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 1, 1 January 2010, Pages 322-325

A series of 4-aminoquinoline–triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum.

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