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aminoquinoline

NOT Open Access | Synthesis and comparison of antiplasmodial activity of (+), (−) and racemic 7-chloro-4-(N-lupinyl)aminoquinoline

September 19, 2012 - 12:55 -- Kabogo Ndegwa
Author(s): 
Chiara Rusconi, Nadia Vaiana, Manolo Casagrande, Nicoletta Basilico, Silvia Parapini, Donatella Taramelli, Sergio Romeo, Anna Sparatore
Reference: 
Bioorganic & Medicinal Chemistry, Volume 20, Issue 19, 1 October 2012, Pages 5980–5985

MalariaWorldRecently the N-(−)-lupinyl-derivative of 7-chloro-4-aminoquinoline ((−)-AM-1; 7-chloro-4-{N-[(1S,9aR)(octahydro-2H-quinolizin-1-yl)methyl]amino}quinoline) showed potent in vitro and in vivo activity against both Chloroquine susceptible and resistant strains of Plasmodium falciparum.

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NOT Open Access | Synthesis and antiplasmodial activity of new heteroaryl derivatives of 7-chloro-4-aminoquinoline

September 19, 2012 - 12:45 -- Kabogo Ndegwa
Author(s): 
Manolo Casagrande, Anna Barteselli, Nicoletta Basilico, Silvia Parapini, Donatella Taramelli, Anna Sparatore
Reference: 
Bioorganic & Medicinal Chemistry, Volume 20, Issue 19, 1 October 2012, Pages 5965–5979

MalariaWorldWith the aim to investigate the effect of different heterocyclic rings linked to the 4-aminoquinoline nucleus on the antimalarial activity, a set of 7-chloro-N-(heteroaryl)-methyl-4-aminoquinoline and 7-chloro-N-(heteroaryl)-4-aminoquinoline was synthesized and tested in vitro against D-10 (CQ-S) and W-2 (CQ-R) strains of Plasmodium falciparum.

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CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline, anti-malarial drug primaquine

August 7, 2012 - 11:46 -- Kabogo Ndegwa
Author(s): 
Pybus BS, Sousa JC, Jin X, Ferguson JA, Christian RE, Barnhart R, Vuong C, Sciotti RJ, Reichard GA, Kozar MP, Walker LA, Ohrt C, Melendez V
Reference: 
Malaria Journal 2012, 11:259 (2 August 2012)

MalariaWorldAs a result of this work, CYP 2D6 and MAO-A have been implicated as the key enzymes associated with PQ metabolism, and metabolites previously identified as potentially playing a role in efficacy and haemolytic toxicity have been attributed to production via CYP 2D6 mediated pathways.

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Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids

March 9, 2011 - 08:13 -- Kabogo Ndegwa
Author(s): 
Marli C. Lombard, David D. N’Da, Jaco C. Breytenbach, Peter J. Smith, Carmen A. Lategan
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 21, Issue 6, 15 March 2011, Pages 1683-1686c

Dihydroartemisinin (DHA) was coupled to different aminoquinoline moieties forming hybrids 9–14, which were then treated with oxalic acid to form oxalate salts (9a–14a).

Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds

November 16, 2010 - 11:33 -- Kabogo Ndegwa
Author(s): 
Eric M. Guantai, Kanyile Ncokazi, Timothy J. Egan, Jiri Gut, Philip J. Rosenthal, Peter J. Smith, Kelly Chibale
Reference: 
Bioorganic & Medicinal Chemistry, Volume 18, Issue 23, 1 December 2010, Pages 8243-8256

A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline and nucleoside templates was synthesized and evaluated for in vitro antimalarial activity. The Cu(I)-catalyzed cycloaddition of azides and terminal alkynes was applied as the hybridization strategy.

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