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The synthesis and metabolism of novel 4-aminoquinoline antimalarials [PDF]
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[Resistance of falciparum malaria to 4-aminoquinolines].
R, Martínez Rodríguez +4 more
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Synthesis of Highly Functionalized 4‐Aminoquinolines
Angewandte Chemie International Edition, 2016AbstractA diverse set of highly substituted 4‐aminoquinolines was synthesized from ynamides, triflic anhydride, 2‐chloropyridine, and readily accessible amides in a mild one‐step procedure.
Tim Wezeman +3 more
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Three 4-aminoquinolines of antimalarial interest
Acta Crystallographica Section C Crystal Structure Communications, 2006The structures of three compounds with potential antimalarial activity are reported. In N,N-diethyl-N'-(7-iodoquinolin-4-yl)ethane-1,2-diamine, C15H20IN3, (I), the molecules are linked into ribbons by N-H...N and C-H...N hydrogen bonds. In N-(7-bromoquinolin-4-yl)-N',N'-diethylethane-1,2-diamine dihydrate, C15H20BrN3.2H2O, (II), two aminoquinoline ...
Susan A, Bourne +2 more
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Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline [PDF]
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.
A. Sparatore +7 more
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4-Aminoquinoline-ferrocene Hybrids as Potential Antimalarials
Recent Patents on Anti-Infective Drug Discovery, 2020Background: Malaria is a deadly disease. It is mostly treated using 4- aminoquinoline derivatives such as chloroquine etc. because it is well-tolerated, displays low toxicity, and after administration, it is rapidly absorbed. The combination of 4-aminoquinoline with other classes of antimalarial drugs has been reported to be an effective approach for ...
Xhamla Nqoro, Blessing A. Aderibigbe
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Synthesis of novel fluorinated 4-aminoquinoline derivatives
Tetrahedron Letters, 2005AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access the actual ChemInform Abstract, please click on HTML or PDF.
Maurice Medebielle +4 more
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Antiplasmodial activities of 4-aminoquinoline–statine compounds
Bioorganic & Medicinal Chemistry Letters, 2012We report the discovery of new potent inhibitors of the growth of Plasmodium falciparum chloroquine (CQ)-resistant W2 strain. These compounds were designed using the double drug approach by introducing a residue able to enhance the accumulation of plasmepsins inhibitors into the food vacuole.
N. Vaiana +11 more
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Pharmacologic actions of 4-aminoquinoline compounds
The American Journal of Medicine, 1983The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye.
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Antimalarial 4‐aminoquinolines: mode of action and pharmacokinetics
Fundamental & Clinical Pharmacology, 1994Summary— In the last ten years, the widespread increase in Plasmodium falciparum resistance to chloroquine has prompted research into antimalarial 4‐aminoquinolines, empirically used up to now. The mechanism of action of 4‐aminoquinolines is characterized by the concentration of the drug in the digestive vacuole of the intraerythrocytic parasite ...
E, Pussard, F, Verdier
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