Pyronaridine

Pyrometric cones Pyrometry Pyronaridine [74847-35-1] Pyromne B [2150-48-3] Pyromne G Pyrophosphatases Pyrophosphates... 

Quinacrine (49) is an acridine that was used extensively from the mid-1920s to the end of World War 11. It acts much like chloroquine and is reasonably effective. Because it causes the skin to turn yellow and, in high doses, causes yellow vision, the dmg is no longer in use as an antimalarial. Pyronaridine (77), a 1-azaacridine developed in China, appears to be effective against mefloquine-resistant, but not entirely against chloroquine-resistant, strains of P falciparum. 

Pyromucic acid — see Furan-2-carboxylic acid Pyronaridine biological activity, 2, 625... 

Naisbitt DJ et al. Metabolism-dependent neutrophil cytotoxicity of amodiaquine A comparison with pyronaridine and related antimalarial drugs. Chemical Research in Toxicology, 1998, 11 1586-1595. 

Evaluation of quinacrine (mepacrine, 22), acrichin N5 (23), acrichin N8 (24), acranil (25), aminoquinacrine (26), desmethoxyquinacrine-N-oxide (27), azacrine (28), pyronaridine (29) and dabequine (30) against Plasmodium infections in experimental animals and humans provided encouraging results. Although desmethoxyquinacrine-N-oxide and azacrine exhibited an activity profile very similar to quinacrine, none offered any distinct advantage over quinacrine [8,16]. 

In the last few years, variations on the basic stracmre have been launched in combination with other antimalarials (usually variations on the chloroquine structure) such as dihydroartemismin and piperaquine phosphate (Artekin), artemether and lumefantrine (Coartem), artesunate/mefloquine (Artequin) and artesunate, sulfamethoxypyrazine, and pyrimethamine (Co-Arinate). Currently, there is another fixed dose combination with an artemisinin derivative in clinical trials, pyronaridine/artesunate (Pyramax in Phase III). However, the tri-oxo scaffold system in artemisinins has led to the synthesis of not only artemisinin variations but to totally synthetic molecules with the trioxane moiety included, such as arterolane tosylate (81). This compound is in Phase II trials as a single agent under Ranbaxy and is in Phase I trials in combination with piperaquine phosphate, also under Ranbaxy. 

Fu, S. Bjorkman, A. Wahlin, B. Ofori-Adjei, D. Ericsson, O. Sjoqvist, F. In vitro activity of chloroquine, the two enantiomers of chloroquine, desethylchloroquine and pyronaridine against Plasmodium falciparum. Br. J. Clin. Pharmacol. 1986, 22, 93-96. 

Figure 6.26 Amodiaquine, pamaquine, primaquine, carboxyprimaquine, WR6026 and pyronaridine.

S.A. Wages, L.C. Patchen and F.C. Churchill, Analysis of blood and urine samples from Macaca mulata for pyronaridine by high-performance liquid chromatography with electrochemical detection, J. Chromatogr., 1990, 527, 115-126. 

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