Disease relevance of NSC7944

• 8-Aminoquinoline toxicity, as measured in the Rane mouse screen, was reduced, and these compounds showed significant blood schizonticidal antimalarial activity in mice [1].
• Phase 2 efficacy trial of an oral 8-aminoquinoline (WR6026) for treatment of visceral leishmaniasis [2].
• The 8-aminoquinoline compound, primaquine, is one of the only compounds useful for relapses of Plasmodium vivax and Plasmodium ovale malaria [3].
• The observation that none of the four test subjects in this study had relapses has not previously been published and may have important implications for the evaluation of other 8-aminoquinoline compounds against relapsing vivax malaria [4].
• Primaquine, an 8-aminoquinoline is also given to patients with falciparum malaria, in a single, 45-mg dose, to kill the gametocytes and so reduce transmission [5].

High impact information on NSC7944

• Tafenoquine is a new 8-aminoquinoline with a much longer half-life than primaquine [6].
• Pure copolymer nanoparticles from 8-aminoquinoline (AQ) and 2-ethylaniline (EA) were easily synthesized by a chemically oxidative polymerization in three different aqueous media [7].
• WR 238605 is an 8-aminoquinoline developed for the radical cure of Plasmodium vivax [8].
• WR 6026 is an 8-aminoquinoline with activity against Pneumocystis carinii in vitro and in an animal model of P. carinii pneumonia that has predicted the clinical utility of related compounds [9].
• Metabolism of a potential 8-aminoquinoline antileishmanial drug in rat liver microsomes [10].

Biological context of NSC7944

• Considerations about the structure-activity relationships of 8-aminoquinoline antimalarial drugs [11].
• Side-chain hydroxylation in the metabolism of 8-aminoquinoline antiparasitic agents [12].
• We studied the pharmacokinetics and pharmacodynamics (percentage methemoglobin) for WR242511, an 8-aminoquinoline primaquine replacement and potential anticyanide compound [3].
• The novel 8-aminoquinoline analogs may have broader utility in public health as future antiprotozoals [13].
• Primaquine, an 8-aminoquinoline, and chloroquine, a 4-aminoquinoline, both stimulate ATP hydrolysis in human red blood cells incubated in the absence of glucose [14].

Anatomical context of NSC7944

• The widely used 8-aminoquinoline antimalarial group of compounds and the derivatives such as WR242511 that are being developed for possible prophylactic anticyanide applications have complex interactions with erythrocytes [15].

Associations of NSC7944 with other chemical compounds

• The 8-aminoquinoline derivatives after nitrite treatment at 5-20 mM for 5 min at pH 3, on the contrary, showed clear mutagenicity in TA100 and WP2uvrA/pKM101 in the presence and absence of S9 mix [16].
• In evaluating the system, pyrimethamine and cycloguanil (dihydrofolate reductase inhibitors) and primaquine (8-aminoquinoline) were tested against pyrimethamine-sensitive and pyrimethamine-resistant strains of Plasmodium falciparum [17].
• Primaquine, an 8-aminoquinoline, was covalently coupled onto oxidized gum arabic via an imine bond and simultaneously fabricated into microspheres of less than 2 microm in size by heat denaturation in a reverse emulsion of 1:1 light paraffin oil and toluene stabilized by sorbitan sesquioleate as the surfactant [18].

Gene context of NSC7944

• Tafenoquine is a promising new 8-aminoquinoline drug that may be useful for malaria prophylaxis in nonpregnant persons with normal glucose-6-phosphate dehydrogenase (G6PD) function [19].

Analytical, diagnostic and therapeutic context of NSC7944

• Development and validation of a stability-indicating reversed-phase high performance liquid chromatography method for NPC 1161C, a novel 8-aminoquinoline anti-malarial drug [20].
• The chemotherapy of rodent malaria. LI. Studies on a new 8-aminoquinoline, WR 238,605 [21].
• Gas chromatography mass spectrometry studies on biologically important 8-aminoquinoline derivatives [22].
• Few studies of phase II clinical trials mainly conducted in Kenya with another drug, sitamaquine or kalazaquine (WR 6026), an 8-aminoquinoline has also shown promise as an orally effective agent (in a dose of 1 mg/kg/day for two weeks) for visceral leishmaniasis [23].

References