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Mefloquine, a clinically useful quinolinemethanol antimalarial which does not significantly bind to DNA

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Abstract

WE report that mefloquine (2,8-bis-(trifluoromethyl)-α-(2-pipe-ridyl)-4-quinolinemethanol1, see Fig. 1) clinically useful against drug-resistant Plasmodium falciparum malaria (G. M. Trenholme, unpublished), does not significantly bind to calf thymus DNA. This constitutes the first reported case of an active compound in the quinoline–acridine class of antimalarials which does not strongly bind to DNA by intercalation.

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Authors and Affiliations

  1. Department of Chemistry, Georgia State University, University Plaza, Atlanta, Georgia, 30303

    MICHAEL W. DAVIDSON, BILLY G. GRIGGS JR, DAVID W. BOYKIN & W. DAVID WILSON

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  1. MICHAEL W. DAVIDSON
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  2. BILLY G. GRIGGS JR
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  3. DAVID W. BOYKIN
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  4. W. DAVID WILSON
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DAVIDSON, M., GRIGGS, B., BOYKIN, D. et al. Mefloquine, a clinically useful quinolinemethanol antimalarial which does not significantly bind to DNA. Nature 254, 632–634 (1975). https://doi.org/10.1038/254632a0

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  • DOI: https://doi.org/10.1038/254632a0

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