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see Fig. 1) clinically useful against drug-resistant Plasmodium falciparum malaria (G. M. Trenholme, unpublished), does not significantly bind to calf thymus DNA.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.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
Receive 51 print issues and online access
$199.00 per year
only $3.90 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
Similar content being viewed by others
References
Ohnmacht, C. J., Patel, A. R., and Lutz, R. E., J. med. Chem., 14, 926–928 (1971).
Lerman, L. S., Proc. natn. Acad. Sci. U.S.A., 49, 94–102 (1963).
Krey, A. K., and Hahn, F. E., Molec. Pharmac., 10, 686–695 (1974).
Pinder, R. M., Medicinal Chemistry third edit., (edit. by Burger, A.), 492–521 (Wiley-Interscience, New York, 1970).
Hahn, F. E., O'Brien, R. L., Ciak, J., Allison, J. L., and Olenick, J. G., Military Med., 131, 1071–1089 (1966).
Carter, G., and Van Dyke, K., Proc. helminth. Soc. Wash., 39 (special issue), 244–249 (1972).
Peters, W., Postgrad. med. J., 49, 573–583 (1973).
Howells, R. E., Peters, W., Homewood, C. A., and Warhurst, D. C., Nature 228, 625–628 (1970). Warhurst, D. C., Homewood, C. A., Peters, W., and Baggaley, V. C., Proc. helminth. Soc. Wash., 39 (special issue), 271–279 (1972).
Steck, E. A., Chemotherapy of Protozoan Diseases, 23, 77–23, 177 (US Government, Washington, DC, 1972).
Peters, W., Chemotherapy and Drug Resistance in Malaria, 12 (Academic, London, (1970).
Panter, J. W., Boykin, D. W., and Wilson, W. D., J. med. Chem., 16, 1366–1369 (1973).
Olmstead, E. J., Panter, J. W., Boykin, D. W., and Wilson, W. D., Biochemistry, 14, 521–526 (1975).
Hahn, F. E., and Fean, C. L., Antimicrob. Ag. Chemother., 63–66 (1969).
Muller, W., Crothers, D. M., and Waring, M. J., Eur. J. Biochem., 39, 223–234 (1973).
Gabbay, E. J., Glasser, R., and Gaffney, B. L., Ann. N. Y. Acad. Sci., 171, 810–825 (1970).
Cohen, S. N., and Yielding, K. L., J. biol. Chem., 240, 3123–3131 (1965).
Colwell, W. T., Brown, V., Christie, P., Lange, J., Reece, C., Yamamoto, K., and Henry, D. W., J. med. Chem., 15, 771–775 (1972).
Cheng, C. C., J. Pharmaceut. Sci., 60, 1596–1597 (1971).
Henry, D. W., Natn. med. chem. Symp. Am. chem. Soc. Proc., 13, 41–50 (1972).
Das, B. P., Nuss, M. E., and Boykin, D. W., J. med. Chem., 17, 516–519 (1974).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
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
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1038/254632a0
This article is cited by
-
Binding of antimalarial drugs to hemozoin fromPlasmodium berghei
Experientia (1980)
Comments
By submitting a comment you agree to abide by our Terms and Community Guidelines. If you find something abusive or that does not comply with our terms or guidelines please flag it as inappropriate.