Photooxidation products of primaquine. Structure, antimalarial activity and hemolytic effects |
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| Authors: | A Brossi W Gessner C D Hufford J K Baker F Homo P Millet I Landau |
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| Institution: | Medicinal Chemistry Section, NIDDK, Bethesda, MD 20892. |
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| Abstract: | Photooxidation of primaquine (1) and 5-hydroxyprimaquine (5) afforded a blue dye for which o-quinone structure 4 was elaborated. Similar oxidation of N-ethoxyacetylprimaquine (10) afforded o-quinone 11. Tissue schizontocidal activity of 4 and 11, and bisquinolylmethine 3 prepared earlier, showed that none of them had noteworthy antimalarial activity, but all three produced methemoglobin. |
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