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- W3174443819 abstract "8-aminoquinolines (8-AQ) are antimalarial drugs that also hold promise for treatment of other infectious diseases. Primaquine is the prototype of the class, and currently the only drug available for relapsing (P. vivax) malaria. Use of 8-AQ is restricted in population with glucose 6-phoshate dehydrogenase deficiency due to hematological toxicity. Biotransformation of 8-aminoquinolines is considered critical for the hematologic effects, but the exact mechanism is not known, largely because of the highly unstable nature of the intermediates generated. An in vitro metabolism-linked human erythrocyte assay has been standardized to evaluate the property of 8-AQs to generate methemoglobin. Direct incubation of drug with microsomes or recombinant human CYP isoforms afforded in situ generation of methemoglobinemic metabolites that mediate a robust hemoglobin oxidation. A series of 5-phenoxy substituted 8-AQ analogs all showed metabolism-mediated methemoglobin formation; various substitutions on the 5-phenoxy ring did not result in significant changes in activity. Removal of the 5-phenoxy ring results in enhanced toxicity. Both carboxyprimaquine and 4-methyl primaquine also showed significant methemoglobin formation. The assay proves useful in generating QSAR data for the class, and can assist in the development of analogs with reduced toxicity. Supported by Medicines for Malaria Venture, Geneva." @default.
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- W3174443819 date "2006-03-01" @default.
- W3174443819 modified "2023-09-27" @default.
- W3174443819 title "An in vitro assay for metabolism‐mediated methemoglobin generation: Evaluation of 8‐aminoquinoline analogs" @default.
- W3174443819 doi "https://doi.org/10.1096/fasebj.20.4.a658-c" @default.
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